Prostigmin


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naproxen sodium

Amerge, Naramig (UK)(Tysabri)StarlixBystolicArranon, Atriance (UK)ViraceptNeo-Fradin, Nivemycin (UK)Prostigmin

Pharmacologic class: Nonsteroidal anti-inflammatory drug (NSAID)

Therapeutic class: Nonopioid analgesic, antipyretic, anti-inflammatory

Pregnancy risk category B (first and second trimesters) D (third trimester)

Pregnancy risk category B (first and second trimesters) D (third trimester)

Pharmacologic class: Selective 5-hydroxytryptamine1 (5-HT1) agonist

Therapeutic class: Vascular headache suppressant, antimigraine drug

Pregnancy risk category C

Pharmacologic class: Recombinant humanized IgG4K monoclonal antibody

Therapeutic class: Immunologic agent

Pregnancy risk category C

Pharmacologic class: Amino acid derivative

Therapeutic class: Hypoglycemic

Pregnancy risk category C

Pharmacologic class: Beta-adrenergic blocker

Therapeutic class: Antihypertensive

Pregnancy risk category C

Pharmacologic class: Phenylpiperazine

Therapeutic class: Antidepressant

Pregnancy risk category C

Pharmacologic class: Antimetabolite

Therapeutic class: Antineoplastic

Pregnancy risk category D

Pharmacologic class: Protease inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category B

Pharmacologic class: Aminoglycoside

Therapeutic class: Anti-infective

Pregnancy risk category D

FDA Box Warning

Drug increases risk of progressive multifocal leukoencephalopathy (PML), an opportunistic viral infection of the brain that usually leads to death or severe disability.

Monitor patient and withhold drug immediately at first sign or symptom suggestive of PML.

Drug is available only through a special restricted distribution program, TOUCH® Prescribing Program, and must be administered only to patients enrolled in this program.

Action

Unknown. Thought to inhibit prostaglandin synthesis.

Availability

naproxen

Oral suspension: 125 mg/5 ml

Tablets: 250 mg, 375 mg, 500 mg

Tablets (delayed-release): 375 mg, 500 mg

naproxen sodium

Caplets, tablets: 220 mg, 275 mg, 550 mg

Tablets (controlled-release): 375 mg, 500 mg, 750 mg

Indications and dosages

Pain; osteoarthritis; ankylosing spondylitis; dysmenorrhea; bursitis; acute tendinitis

Adults: 250 to 500 mg (naproxen) P.O. b.i.d. (up to 1.5 g/day); 375 to 500 mg (naproxen delayed-release) P.O. t.i.d.; 250 mg, 375 mg, or 500 mg (naproxen oral suspension) P.O. b.i.d.; 275 to 550 mg (naproxen sodium) P.O. b.i.d. (up to 1.65 g/day)

Children: 10 mg/kg P.O. daily in two divided doses (naproxen only)

Mild to moderate pain; primary dysmenorrhea

Adults: Initially, 500 mg (naproxen) P.O., followed by 250 mg q 6 to 8 hours p.r.n., to a maximum of 1.25 g/day. Or initially, 550 mg (naproxen sodium) P.O., followed by 275 mg q 6 to 8 hours p.r.n., to a maximum of 1,375 mg/day.

Gout

Adults: Initially, 750 mg (naproxen) P.O., followed by 250 mg q 8 hours or initially, 825 mg (naproxen sodium) P.O., followed by 275 mg q 8 hours. On day 1,1,000 to 1,500 mg (naproxen sodium controlled-release formulation) P.O. once daily, followed by 1,000 mg once daily until attack has subsided.

Management of pain, primary dysmenorrhea, acute tendinitis and bursitis

Adults: Initially, two 500-mg naproxen sodium controlled-release tablets P.O. once daily. Or, for patients requiring greater analgesic benefit, two 750-mg naproxen sodium controlled-release tablets P.O. once daily. Or, three 500-mg naproxen sodium controlled-release tablets may be used for a limited period. Thereafter, total daily dose shouldn't exceed two 500-mg tablets.

Rheumatoid arthritis, osteoarthritis, ankylosing spondylitis

Adults: Initially, two 375-mg naproxen sodium controlled-release tablets P.O. once daily, one 750-mg tablet P.O. once daily, or two 500-mg tablets P.O. once daily. During long-term administration, adjust dosage up or down depending on patient's clinical response. Use lowest effective dose in all patients. (Patients already taking naproxen 250 mg, 375 mg, or 500 mg b.i.d. may have their total daily dosage replaced with naproxen sodium controlled-release tablets as a single daily dose.)

Dosage adjustment

• Renal or hepatic impairment
• Elderly patients

Contraindications

• Hypersensitivity to drug or other NSAIDs
• Asthma, urticaria, or allergic-type reactions after taking aspirin or other NSAIDs
• Perioperative pain in the setting of coronary artery bypass graft surgery

Precautions

Use cautiously in:
• severe cardiovascular, renal, or hepatic disease
• advanced renal disease (not recommended)
• history of ulcer disease or GI bleeding (use with extreme caution)
• chronic alcohol use or abuse
• elderly patients
• pregnant patients
• breastfeeding patients (avoid use)
• children (naproxen sodium controlled-release) and naproxen use in children younger than age 2 (safety not established).

Administration

• Give with food or milk to avoid GI upset.

Adverse reactions

CNS: dizziness, drowsiness, headache, vertigo, light-headedness

CV: palpitations, tachycardia, hypertension

GU: renal toxicity (with long-term use in patients in whom renal prostaglandins have a compensatory role in maintenance of renal perfusion), renal papillary necrosis

EENT: visual disturbances, tinnitus, auditory disturbances

GI: nausea, diarrhea, constipation, heartburn, abdominal pain, stomatitis, GI bleeding

Skin: rash, pruritus, skin eruptions, sweating, photosensitivity, exfoliative dermatitis, Stevens-Johnson syndrome, toxic epidermal necrolysis

Other: thirst, edema, allergic reactions including anaphylaxis

Interactions

Drug-drug.Acetaminophen (chronic use), cyclosporine: increased risk of adverse renal effects

Anticoagulants, thrombolytics: increased anticoagulant effect

Antihypertensives, cefamandole, cefoperazone, cefotetan, diuretics, eptifibatide: decreased response

Antineoplastics, methotrexate: increased risk of nephrotoxicity

Aspirin: decreased naproxen efficacy

Aspirin, corticosteroids, other NSAIDs: additive adverse GI effects

Clopidogrel, plicamycin, ticlopidine, valproic acid: increased risk of bleeding Insulin, oral hypoglycemics: increased risk of hypoglycemia

Lithium: increased lithium blood level and risk of nephrotoxicity

Other photosensitizing agents: increased risk of photosensitivity

Probenecid: increased naproxen blood level, increased risk of toxicity

Drug-diagnostic tests.Alanine amino-transferase, alkaline phosphatase, aspartate aminotransferase, blood urea nitrogen, creatinine, lactate dehydroge-nase, potassium: increased levels

Bleeding time: prolonged for up to 4 days after therapy ends

Creatinine clearance, glucose, hematocrit, hemoglobin, leukocytes, platelets: decreased values

Urine 5-hydroxy-indoleacetic acid, urine steroids: test interference

Drug-herbs.Anise, arnica, chamomile, clove, dong quai, fenugreek, feverfew, garlic, ginger, ginkgo, ginseng, licorice: increased anticoagulant effect, increased risk of bleeding

Patient monitoring

• Monitor GI status. Stay alert for signs and symptoms of GI bleeding.

In long-term use, assess CBC with white cell differential and coagulation studies, and monitor for visual and hearing impairment and renal toxicity.
• Monitor cardiovascular status for tachycardia, palpitations, hypertension, and edema.
• Monitor blood glucose level closely in diabetic patients.

Monitor patient for signs and symptoms of serious skin manifestations; discontinue drug at first appearance of rash or other signs of hypersensitivity.

Patient teaching

• Tell patient to take medication with food or milk followed by 8 oz of water, and to stay upright for 30 minutes afterward.
• Inform patient that he may crush or break regular tablets but must swallow delayed- or controlled-release form whole.
• Tell patient that drug's full therapeutic effect may take up to 2 weeks.
• Caution patient not to exceed recommended dosage.

Instruct patient how to recognize and immediately report signs and symptoms of renal toxicity and serious skin manifestations.
• Advise patient to use sunscreen to prevent photosensitivity reaction.
• Instruct patient not to take over-the-counter medications unless prescribed.
• Tell patient to consult prescriber before taking herbs.
• Advise female patient to tell prescriber if she is pregnant or breastfeeding before starting drug.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.


naratriptan hydrochloride

Amerge, Naramig (UK)


Pharmacologic class: Selective 5-hydroxytryptamine1 (5-HT1) agonist

Therapeutic class: Vascular headache suppressant, antimigraine drug

Pregnancy risk category C

 

Action

Binds with specific 5-HT1 receptors in intracranial blood vessels and sensory trigeminal nerves, leading to vasoconstriction and migraine relief

Availability

Tablets: 1 mg, 2.5 mg

Indications and dosages

Migraine headache

Adults: 1 or 2.5 mg P.O. as single dose; may repeat in 4 hours. Don't exceed 5 mg in 24 hours; don't use to treat more than four headaches per month.

Dosage adjustment

• Mild to moderate renal or hepatic impairment

Contraindications

• Hypersensitivity to drug or its components
• Hemiplegic or basilar headaches
• Severe renal, cardiovascular or hepatic impairment
• History of cerebrovascular or peripheral vascular conditions
• Ischemic bowel disease
• Uncontrolled hypertension
• Use of ergot-type drugs (such as dihydroergotamine) and other 5-HT1 agonists within 24 hours
• MAO inhibitor use within past 14 days

Precautions

Use cautiously in:
• mild to moderate renal or hepatic impairment, cardiovascular risk factors
• elderly patients (not recommended)
• pregnant or breastfeeding patients
• children (safety not established).

Administration

• Know that drug does not prevent migraine.
• Give only if patient's cardiovascular status has been evaluated and determined to be safe, and if first dose can be given under supervision.

Adverse reactions

CNS: dizziness, drowsiness, malaise, fatigue, paresthesia, cerebral hemorrhage, subarachnoid hemorrhage, stroke, other cerebrovascular events

CV: significant blood pressure elevation including hypertensivecrisis (rare), coronary artery vasospasm, myocardial infarction, ventricular fibrillation or tachycardia

GI: nausea, vomiting, colonic ischemia with abdominal pain, bloody diarrhea

Other: pain or pressure sensation in throat or neck, peripheral vascular ischemia, serotonin syndrome, hypersensitivity including anaphylaxis or anaphylactoid reactions

Interactions

Drug-drug.Ergot-type compounds (dihydroergotamine, methysergide): prolonged vasospastic reaction

Hormonal contraceptives: increased naratriptan blood level and effects

MAO inhibitors: increased systemic exposure to naratriptan, increased risk of adverse reactions

Selective serotonin reuptake inhibitors: weakness, hyperreflexia, incoordination Sibutramine: serotonin syndrome

Drug-herbs.S-adenosylmethionine (SAM-e), St. John's wort: increased risk of adverse serotonergic effects

Drug-behaviors.Cigarette smoking: increased naratriptan metabolism

Patient monitoring

• Maintain especially close monitoring in patients with cardiovascular risk factors (such as hypertension, hypercholesterolemia, obesity, diabetes mellitus, cigarette smoking, strong family history), postmenopausal women, and men older than age 40.
• Assess vital signs and ECG.
• Monitor neurologic status closely. Institute safety measures as needed to prevent injury.

Discontinue drug if serotonin syndrome is suspected.

Patient teaching

• Tell patient to take at first sign of headache.
• Advise patient to take second dose (if approved) at least 4 hours after first dose if headache has not gone away completely or has returned.
• Caution patient not to take more than two tablets in a 24-hour period.

Instruct patient how to recognize and immediately report signs and symptoms of stroke and other neurologic conditions, serotonin syndrome, hypersensitivity, or bloody diarrhea.
• Advise patient to avoid driving and other hazardous activities until he knows how drug affects concentration and alertness.
• Tell patient to avoid cigarette smoking and to discuss herb use with prescriber.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors mentioned above.


natalizumab

(Tysabri)


Pharmacologic class: Recombinant humanized IgG4K monoclonal antibody

Therapeutic class: Immunologic agent

Pregnancy risk category C

 

FDABOXED WARNING

Drug increases risk of progressive multifocal leukoencephalopathy (PML), an opportunistic viral infection of the brain that usually leads to death or severe disability.

Monitor patient and withhold drug immediately at first sign or symptom suggestive of PML.

Drug is available only through a special restricted distribution program, TOUCH® Prescribing Program, and must be administered only to patients enrolled in this program.

Action

Binds to the α4-subunit of α4β1 and α4β7 integrins expressed on the surface of all leukocytes except neutrophils, and inhibits the α4-mediated adhesion of leukocytes to their counterreceptor(s). The receptors for the α4 family of integrins include vascular cell adhesion molecule-1 (VCAM-1), which is expressed on activated vascular endothelium, and mucosal address in cell adhesion molecule-1 (MAdCAM-1) present on vascular endothelial cells of the GI tract. Disruption of these molecular interactions prevents transmigration of leukocytes across the endothelium into inflamed parenchymal tissue. Specific mechanisms by which drug exerts its effects in multiple sclerosis (MS) and Crohn's disease haven't been fully defined.

Availability

Solution for infusion: 300 mg/15-ml vial (20 mg/ml)

Indications and dosages

Relapsing forms of MS; moderately to severely active Crohn's disease in patients with evidence of inflammation who have had inadequate response to or can't tolerate conventional therapy

Adults: 300 mg by I.V. infusion over approximately 1 hour q 4 weeks. In Crohn's disease, discontinue in patient who hasn't experienced therapeutic benefit by 12 weeks of induction therapy and in patient who can't discontinue long-term concomitant steroids within 6 months of starting natalizumab.

Contraindications

• Hypersensitivity to drug
• History of or current PML

Precautions

Use cautiously in:
• hepatic impairment
• infections, immune reconstitution inflammatory syndrome
• concurrent use of TNFa inhibitors, antineoplastics, prolonged immunosuppressant or immunomodulatory therapy; systemic medical condition resulting in significantly compromised immune system (avoid use)
• pregnant or breastfeeding patients
• children younger than age 18 (safety and efficacy not established).

Administration

Don't give as I.V. push or bolus.
• To prepare solution, withdraw 15 ml of drug concentrate from vial. Inject concentrate into 100 ml 0.9% sodium chloride injection, leading to concentration of 2.6 mg/ml. Don't use other I.V. diluents or mix with other drugs. Gently invert vial to mix completely; don't shake. Following dilution, infuse solution immediately or refrigerate at 2° to 8° C (36° to 46° F), and use within 8 hours.
• Infuse 300 mg in 100 ml 0.9% sodium chloride injection over approximately 1 hour (infusion rate approximately 5 mg/minute). After infusion is complete, flush with 0.9% sodium chloride injection.

Observe patient during infusion and for 1 hour after infusion is complete. Promptly discontinue infusion at first sign or symptom consistent with a hypersensitivity reaction.

Obtain MRI scan in MS patients before starting therapy to help differentiate subsequent MS signs and symptoms from those of PML. Withhold drug immediately at first sign or symptom suggestive of PML.

• Be aware that a baseline brain MRI in patients with Crohn's disease may help distinguish preexisting lesions from newly developed lesions.

For patients with Crohn's disease who start drug while taking long-term corticosteroids, start steroid withdrawal as soon as therapeutic benefit has occurred. If patient can't discontinue systemic corticosteroids within 6 months, discontinue natalizumab.

Discontinue drug in patients with jaundice or other evidence of significant liver injury.

Adverse reactions

CNS: headache, fatigue, depression, somnolence, vertigo, tremor, PML

EENT: tonsillitis, pharyngolaryngeal pain, sinusitis

GI: nausea, diarrhea, constipation, dyspepsia, gastroenteritis, abdominal discomfort, flatulence, aphthous stomatitis, exacerbation of Crohn's disease, intestinal obstruction or stenosis

GU: vaginitis; irregular menstruation; dysmenorrhea; amenorrhea; ovarian cyst; urinary tract infection; urinary incontinence, urgency, frequency

Hepatic: abnormal liver function test values

Musculoskeletal: arthralgia, extremity pain, back pain, muscle cramps, joint swelling, limb injury

Respiratory: upper and lower respiratory tract infections, cough

Skin: rash, dermatitis, pruritus, urticaria, dry skin, skin laceration, thermal burn

Other: infections, chest discomfort, seasonal allergy, weight changes, tooth infections, toothache, herpes infection, night sweats, rigors, peripheral edema, influenza-like illness, immunosuppression, infusion reactions, hypersensitivity reactions including anaphylaxis

Interactions

Drug-drug.Corticosteroids, immunosuppressants (such as azathioprine, cyclosporine, 6-mercaptopurine, methotrexate), TNFα inhibitors: increased risk of PML and other infections

Drug-diagnostic tests.Circulating basophils, eosinophils, lymphocytes, monocytes, nucleated RBCs: increased levles

Hemoglobin: decreased level

Patient monitoring

• Monitor CBC with differential and hepatic function tests.

Continue to monitor patient for hypersensitivity reactions; infection; hepatotoxicity; signs and symptoms of immune reconstitution inflammatory syndrome (including unanticipated clinical decline in patient's condition after return of immune function and in some cases after apparent clinical improvement; and PML signs and symptoms (such as progressive weakness on one side of the body, limb clumsiness, vision disturbances, and changes in thinking, memory, and orientation leading to confusion and personality changes).

Patient teaching

• Explain the TOUCH Prescribing Program to patient.

Instruct patient to immediately report hypersensitivity reactions (such as flushing, nausea, headache, dizziness, fatigue, hives, or itching); signs and symptoms of infections; signs and symptoms of hepatotoxicity (such as yellowing of skin or eyes, dark urine, or right upper abdominal pain or discomfort); unanticipated clinical decline in condition or new signs and symptoms; or signs and symptoms of PML (such as progressive weakness on one side of the body, limb clumsiness, vision disturbances, and changes in thinking, memory, and orientation leading to confusion and personality changes).
• Instruct patient to tell prescriber about all drugs he's taking, because some drugs have potential for serious drug interactions and shouldn't be taken with natalizumab.
• Advise female patient of childbearing age that drug should be used during pregnancy only if potential benefit justifies potential risk to fetus.
• Advise breastfeeding patient that she should decide whether to discontinue breastfeeding or discontinue drug, taking into account importance of drug for her treatment.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.


nateglinide

Starlix


Pharmacologic class: Amino acid derivative

Therapeutic class: Hypoglycemic

Pregnancy risk category C

 

Action

Decreases blood glucose level by stimulating insulin secretion from pancreatic beta cells; interacts with calcium and potassium channels in pancreas

Availability

Tablets: 60 mg, 120 mg

Indications and dosages

To decrease glucose levels in type 2 (non-insulin-dependent) diabetes mellitus not adequately controlled by diet and exercise

Adults: 120 mg P.O. t.i.d. up to 30 minutes before meals, or 60 mg P.O. t.i.d. if patient is near glycosylated hemoglobin (HbA1c) goal

Contraindications

• Hypersensitivity to drug or its components
• Diabetic ketoacidosis
• Type 1 (insulin-dependent) diabetes mellitus

Precautions

Use cautiously in:
• renal or hepatic impairment, adrenal or pituitary insufficiency
• elderly or malnourished patients
• pregnant or breastfeeding patients.

Administration

• Give 30 minutes before meals. If meal is missed, don't give dose.
• Know that drug may be given alone or with metformin.

Adverse reactions

CNS: dizziness

GI: diarrhea

Metabolic: hypoglycemia

Musculoskeletal: back pain, joint pain

Respiratory: upper respiratory tract infection, bronchitis, coughing

Other: flulike symptoms, trauma

Interactions

Drug-drug.Beta-adrenergic blockers, MAO inhibitors, nonsteroidal antiinflammatory drugs, salicylates: increased hypoglycemic effect

Corticosteroids, sympathomimetics, thiazides, thyroid products: reduced hypoglycemic effect

Drug-diagnostic tests.Glucose: decreased level

Patient monitoring

• Monitor blood glucose and HbA1c levels.
• Assess pulmonary status for bronchitis, upper respiratory infection, and flulike signs and symptoms.
• Monitor musculoskeletal status. Check for back pain and arthropathy.
• Note GI complaints, and identify nutritional deficiencies.

Patient teaching

• Instruct patient to take dose up to 30 minutes before each main meal.
• Advise patient not to skip a meal. If he does, tell him to also skip accompanying nateglinide dose, to prevent hypoglycemia.
• Teach patient how to monitor blood and urine for glucose and ketones, as prescribed.
• Instruct patient to report adverse CNS effects and signs and symptoms of respiratory infection.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects sensation and balance.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.


nebivolol

Bystolic


Pharmacologic class: Beta-adrenergic blocker

Therapeutic class: Antihypertensive

Pregnancy risk category C

 

Action

Not fully known. The following factors may be involved: decreased heart rate, reduced myocardial contractility, decreased tonic sympathetic outflow to periphery from cerebrovasomotor centers, suppressed renin activity, vasodilation, and decreased peripheral vascular resistance.

Availability

Tablets: 2.5 mg, 5 mg, 10 mg

Indications and dosages

Hypertension

Adults: Individualized; 5 mg P.O. daily. If patient requires further blood pressure reduction, dosage may be increased at 2-week intervals up to 40 mg P.O. daily.

Dosage adjustment

• Moderate hepatic impairment or severe renal impairment (creatinine clearance less than 30 ml/minute)

Contraindications

• Hypersensitivity to drug or its components
• Severe bradycardia, heart block greater than first degree, cardiogenic shock, decompensated cardiac failure, sick sinus syndrome (unless permanent pacemaker is in place)
• Severe hepatic impairment

Precautions

Use cautiously in:
• moderate hepatic impairment
• severe renal impairment
• congestive heart failure (CHF)
• peripheral vascular disease
• bronchospastic disease (use not recommended)
• diabetic patients receiving hypoglycemic drugs
• known or suspected pheochromocytoma
• concurrent use of myocardial depressants, AV conduction inhibitors (such as cardiac glycosides and certain calcium antagonists), or antiarrhythmics (such as disopyramide)
• perioperative use with anesthetics that depress myocardial function (such as ether, cyclopropane, or trichloroethylene)
• pregnant patients
• breastfeeding patients (use not recommended)
• children (safety and efficacy not established).

Administration

• Give with or without food.
• Be aware that drug may be used alone or in combination with other antihypertensives.
• Know that drug shouldn't be combined with other beta blockers. Closely monitor patients receiving catecholamine-depleting drugs (such as reserpine or guanethidine), because added beta blockade may decrease sympathetic activity excessively. In patients receiving nebivolol with clonidine, discontinue nebivolol for several days before gradually tapering clonidine.

Don't withdraw drug abruptly; taper over 1 to 2 weeks when possible. Drug may mask signs and symptoms of hyperthyroidism, such as tachycardia; abrupt withdrawal may exacerbate signs and symptoms of hyperthyroidism or may trigger thyroid storm.

Adverse reactions

CNS: headache, fatigue, dizziness, insomnia

CV: bradycardia

GI: nausea, diarrhea

Respiratory: dyspnea

Skin: rash

Other: chest pain, peripheral edema

Interactions

Drug-drug.Antiarrhythmics (such as disopyramide), myocardial depressants or AV conduction inhibitors (such as cardiac glycosides and certain calcium antagonists): increased risk of slowed AV conduction and bradycardia

Cimetidine: increased d-nebivolol (active isomer) blood level

CYP2D6 inhibitors (such as fluoxetine, paroxetine, propafenone, quinidine): increased d-nebivolol blood level

Other beta-adrenergic blockers: excessive reduction of sympathetic activity Sildenafil: decreased effect of sildenafil

Drug-diagnostic tests.Blood urea nitrogen, triglycerides, uric acid: increased levels

Cholesterol, high-density lipoproteins, platelet count: decreased

Patient monitoring

Be aware that beta blockade may further depress myocardial contractility and trigger more severe heart failure in patients with compensated CHF. If CHF worsens, consider discontinuing drug.

During perioperative use, closely monitor patients receiving anesthetics that depress myocardial function, such as ether, cyclopropane, or trichloroethylene. Also, know that if drug is withdrawn before major surgery, the heart's impaired ability to respond to reflex adrenergic stimuli may increase risks of general anesthesia and surgery.
• Because of significant negative inotropic and chronotropic effects in patients treated with verapamil- or diltiazem-type beta blockers or calcium channel blockers, use caution in patients treated concomitantly with these agents; monitor ECG and blood pressure.

Patient teaching

• Tell patient drug may be taken with or without food.
• Advise patient not to stop taking drug unless prescriber approves.

Instruct patient to immediately report difficulty breathing, increasing shortness of breath, excessively slow pulse, or weight gain.
• Caution patient to avoid driving and other hazardous activities until drug's effects on alertness are known.
• Advise breastfeeding patient not to breastfeed during therapy.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs and tests mentioned above.


nefazodone hydrochloride

Action

Potentiates effects of norepinephrine and serotonin by blocking synaptic reuptake in nerve cells and disrupting alpha1-adrenergic receptors

Availability

Tablets: 50 mg, 100 mg, 150 mg, 200 mg, 250 mg

Indications and dosages

Major depression

Adults: Initially, 100 mg P.O. b.i.d. May increase weekly up to 600 mg/day in two divided doses.

Dosage adjustment

• Elderly patients

Contraindications

• Hypersensitivity to drug, its components, or other phenylpiperazines
• Active hepatic disease, baseline transaminase elevation, or previous drug withdrawal necessitated by hepatic damage
• MAO inhibitor use within past 14 days
• Concurrent cisapride (not available in U.S.), pimozide, carbamazepine, or triazolam therapy

Precautions

Use cautiously in:
• cardiovascular or cerebrovascular disease
• history of suicide attempt, drug abuse, or mania
• elderly patients
• pregnant or breastfeeding patients
• children younger than age 18 (safety not established).

Administration

• Give with food or milk if GI upset occurs.
• Know that tablets may be crushed.

Don't give concurrently with cisapride, pimozide, carbamazepine, or triazolam.

Don't give within 14 days of MAO inhibitors.

Adverse reactions

CNS: dizziness, asthenia, agitation, light-headedness, insomnia, drowsiness, confusion, weakness, headache, impaired memory, poor concentration, paresthesia, psychomotor retardation, tremor, suicidal behavior or ideation (especially in child or adolescent)

CV: hypotension, orthostatic hypotension, peripheral edema

EENT: abnormal or blurred vision, eye pain, tinnitus, pharyngitis

GI: nausea, vomiting, diarrhea, constipation, dyspepsia, dry mouth

GU: urinary frequency or retention, urinary tract infection

Hepatic: hepatotoxicity, hepatic failure

Respiratory: increased cough

Skin: rash, pruritus

Other: increased appetite, thirst, infection, chills, fever, flulike symptoms

Interactions

Drug-drug.Alprazolam, triazolam: increased blood level and effects of these drugs

Antihypertensives, nitrates: additive hypotension

Carbamazepine, cisapride, pimozide: increased nefazodone blood level, leading to toxicity

CNS depressants (including antihistamines, opioids, sedative-hypnotics): additive CNS depression

Digoxin: increased digoxin blood level

HMG-CoA reductase inhibitors: increased risk of myopathy

MAO inhibitors: potentially fatal reactions (hyperpyrexia, excitation, seizures, delirium, coma)

Drug-diagnostic tests.CBC, cholesterol, glucose, hematocrit: decreased levels

Hepatic enzymes: increased levels

Drug-herbs.Chamomile, hops, kava, skullcap, valerian: increased CNS depression

S-adenosylmethionine (SAM-e), St. John's wort: increased risk of adverse serotonergic effects, including serotonin syndrome

Drug-behaviors.Acute alcohol ingestion: additive hypotension

Alcohol use: increased CNS depression

Patient monitoring

• Monitor vital signs with patient lying down, sitting, and standing. Notify prescriber if blood pressure drops 20 mm Hg.
• Assess CBC.

Monitor liver function tests frequently. Notify prescriber of abnormal results.
• Closely monitor neurologic status.
• Evaluate patient for withdrawal symptoms (which may occur if therapy stops abruptly).

Monitor closely for increasing depression and suicidal ideation (especially in child or adolescent).

Patient teaching

• Advise patient to take with food or milk to minimize GI upset.
• Tell patient to crush drug if he can't swallow it whole.
• Inform patient that therapeutic response may take up to 4 weeks. Encourage him to keep taking drug as prescribed.

Tell patient drug may cause adverse CNS effects. Advise him to report significant mood changes (especially depression or suicidal thoughts). Caution parent to report these problems in child or adolescent.

Instruct patient to immediately report unusual tiredness, yellowing of skin or eyes, nausea, or anorexia.
• Instruct patient to rise slowly and carefully, to avoid dizziness from temporary blood pressure drop.
• Tell patient to avoid alcohol and to consult prescriber before taking herbs.

Instruct patient not to stop taking drug abruptly. Dosage must be tapered.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, herbs, and behaviors mentioned above.


nelarabine

Arranon, Atriance (UK)


Pharmacologic class: Antimetabolite

Therapeutic class: Antineoplastic

Pregnancy risk category D

 

FDABOXED WARNING

Administer I.V. only.

Give under supervision of physician experienced in use of cancer chemotherapy.

Drug has caused severe neurologic events, including severe somnolence, seizures, and peripheral neuropathy. Demyelination-associated events also have occurred. Drug discontinuation doesn't always lead to full recovery from these events. Monitor patient closely for neurologic changes; discontinue drug for serious neurologic events.

Action

Inhibits DNA synthesis in leukemic blasts, leading to cell death

Availability

Solution for injection: 250 mg/50 ml

Indications and dosages

T-cell acute lymphoblastic leukemia and T-cell lymphoblastic lymphoma in patients whose disease hasn't responded to at least two chemotherapy regimens or who've relapsed after such therapy

Adults: 1,500 mg/m2 I.V. undiluted over 2 hours on days 1, 3, and 5; repeat every 21 days. Continue therapy until disease progresses, unacceptable toxicity occurs, patient becomes eligible for bone marrow transplant, or patient no longer benefits from therapy.

Children: 650 mg/m2 I.V. undiluted over 1 hour daily for 5 consecutive days; repeat every 21 days. Continue therapy until disease progresses, unacceptable toxicity occurs, patient becomes eligible for bone marrow transplant, or patient no longer benefits from therapy.

Dosage adjustment

• Neurologic or hematologic toxicity

Contraindications

• Hypersensitivity to drug or its components

Precautions

Use cautiously in:
• renal or hepatic dysfunction
• patients undergoing concurrent intrathecal chemotherapy
• patients previously treated with intrathecal chemotherapy or craniospinal irradiation
• concurrent administration of live vaccines (immunocompromised patients)
• elderly patients
• pregnant or breastfeeding patients.

Administration

• Administer undiluted.
• Infuse over 2 hours in adults or over 1 hour in children.
• In patients at risk for tumor lysis syndrome, take measures to prevent hyperuricemia (such as hydration, urine alkalization, and allopurinol prophylaxis).

Discontinue drug if serious neurologic adverse reactions occur.

Adverse reactions

CNS: confusional state, insomnia, depression, headache, peripheral neuropathy, somnolence, paresthesia, hypoesthesia, fine motor dysfunction, neurologic disorder, tremor, ataxia, abnormal gait, dizziness, amnesia, balance disorder, sensory loss, demyelination, asthenia, fatigue, rigors, decreased level of consciousness, seizures, cerebral hemorrhage, coma

CV: tachycardia, chest pain, hypotension

EENT: blurred vision, epistaxis, sinusitis

GI: nausea, vomiting, diarrhea, constipation, abdominal pain, abdominal distention, stomatitis, anorexia

Hematologic: anemia, neutropenia, thrombocytopenia, leukopenia

Metabolic: dehydration

Musculoskeletal: myalgia, arthralgia, back pain, muscle weakness, extremity pain

Respiratory: pneumonia, cough, dyspnea, exertional dyspnea, wheezing, pleural effusion

Skin: petechiae

Other: abnormal taste, infection, fever, edema, peripheral edema, pain, non-cardiac chest pain

Interactions

Drug-drug.Pentostatin: decreased nelarabine efficacy

Drug-diagnostic tests.Bilirubin, serum creatinine, transaminases: increased

Blood albumin, CBC, calcium, glucose, magnesium, platelets, potassium: decreased

Patient monitoring

Watch closely for neurologic events, such as somnolence, confusion, seizures, ataxia, motor incoordination, and peripheral neuropathy (which may not subside even after therapy ends). Know that previous craniospinal irradiation or current or previous intrathecal chemotherapy may increase patient's risk of adverse neurologic events.
• Closely monitor patients with hepatic or renal dysfunction for adverse reactions.
• Monitor CBC regularly.

Patient teaching

• Instruct patient or caregiver to read patient information leaflet thoroughly.

Urge patient or caregiver to immediately report neurologic symptoms, such as extreme sleepiness, confusion, seizures, unsteadiness or weakness on walking, difficulty with tasks such as buttoning clothing, and numbness and tingling in fingers, hands, or feet.

Tell patient to immediately report easy bruising, bleeding, fever, or signs or symptoms of infection.
• Inform patient that he'll need to undergo frequent blood tests.
• Instruct patient to avoid live virus vaccines.
• Caution patient to avoid driving and other hazardous activities until drug effects are known.
• Urge female with childbearing potential to avoid pregnancy and breastfeeding during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.


nelfinavir mesylate

Viracept


Pharmacologic class: Protease inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category B

 

Action

Inhibits action of human immunodeficiency virus (HIV) protease and prevents cleavage of viral polyproteins, resulting in production of immature, noninfectious virus

Availability

Oral powder: 50 mg/1 g powder (1 g powder/level scoopful)

Tablets: 250 mg, 625 mg

Indications and dosages

HIV infection

Adults and children older than age 13: 750 mg P.O. t.i.d. or 1,250 mg b.i.d., given with other antiretrovirals

Children ages 2 to 13: 20 to 30 mg/kg P.O. t.i.d., given with a meal or light snack

Contraindications

• Hypersensitivity to drug or its components
• Concurrent use of amiodarone, dihydroergotamine, ergonovine, ergotamine, midazolam, pimozide, quinidine, rifampin, sildenafil (when used for pulmonary arterial hypertension), or triazolam

Precautions

Use cautiously in:
• moderate or severe hepatic impairment (avoid use)
• hemophilia, diabetes mellitus
• concurrent use of lovastatin, simvastatin, or St. John's wort (not recommended)
• concurrent use of other HMG-CoA reductase inhibitors also metabolized by the CYP3A pathway, proton pump inhibitors, and rifampin
• phenylketonuria (oral powder contains phenylalanine)
• breastfeeding patients.

Administration

• Give tablets with food.
• For adult who can't swallow tablets whole, crush and mix in food or dissolve in small amount of water. Have patient consume mixture immediately, or refrigerate for up to 6 hours.
• For child who can't swallow tablets, mix oral powder with small amount of water, formula, or milk. Have child consume mixture immediately, or refrigerate for up to 6 hours.
• Don't mix powder with water in its original container.
• Don't mix powder with acidic juice (combination produces bitter taste).

Don't give concurrently with amiodarone, astemizole, cisapride, dihydroergotamine, ergotamine, midazolam, quinidine, rifampin, terfenadine, or triazolam.

Adverse reactions

CNS: anxiety, depression, dizziness, drowsiness, emotional lability, headache, hyperkinesia, insomnia, malaise, migraine headache, sleep disorders, weakness, myasthenia, paresthesia, suicidal ideation, seizures

EENT: acute iritis, rhinitis, sinusitis, pharyngitis

GI: nausea, diarrhea, abdominal pain, flatulence

GU: nephrolithiasis, sexual dysfunction

Hematologic: anemia, leukopenia, thrombocytopenia

Metabolic: dehydration, hyperuricemia, hyperglycemia, hypoglycemia

Musculoskeletal: joint pain, arthritis, back pain, myalgia, myopathy

Respiratory: dyspnea, bronchospasm

Skin: pruritus, rash, sweating, fungal dermatitis, folliculitis, urticaria

Other: fever, body fat redistribution, allergic reactions, immune reconstitution syndrome

Interactions

Drug-drug.Amiodarone, dihydroergotamine, ergotamine, midazolam, quinidine, triazolam: excessive sedation, vasoconstriction, serious arrhythmias

Atorvastatin, rosuvastatin: increased statin concentration

Azithromycin, bosentan, colchicine, inhaled fluticasone, salmeterol: increased concentration of these drugs

Carbamazepine, phenobarbital, phenytoin, rifampin: decreased nelfinavir blood level and efficacy

Delavirdine: increased nelfinavir concentration, decreased delavirdine concentrations

HMG-CoA reductase inhibitors: increased risk of serious reactions, such as myopathy and rhabdomyolysis

Hormonal contraceptives: decreased contraceptive blood level and efficacy

Immunosuppressants (cyclosporine, sirolimus, tacrolimus): increased immunosuppressant concentration

Indinavir, saquinavir: increased indinavir or saquinavir concentration and increased nelfinavir concentration

Methadone, trazodone: decreased concentration of these drugs Nevirapine: decreased nelfinavir concentration

Rifabutin: decreased rifabutin metabolism and effects Ritonavir: increased nelfinavir concentration

Sildenafil, tadalafil, vardenafil: increased risk of adverse events

Warfarin: affected warfarin concentration

Drug-diagnostic tests.Alanine amino-transferase, alkaline phosphatase, amylase, aspartate aminotransferase, creatine kinase, gamma-glutamyl transpeptidase, lactic dehydrogenase lipids, uric acids: increased levels Blood glucose: increased or decreased level

Hemoglobin, platelets, white blood cells: decreased levels

Drug-food.Most foods: enhanced drug absorption

Drug-herbs.St. John's wort: decreased nelfinavir blood level and efficacy

Patient monitoring

Watch for signs and symptoms of depression and suicidal ideation.
• Evaluate neurologic status closely, particularly for seizures and sensori-motor dysfunction.
• Assess CBC, lipid panel, uric acid level, and HIV-specific tests.
• Watch for secondary infections, particularly fungal and EENT infections.

Be aware that immune reconstitution syndrome may occur in patients receiving combination anti-retroviral therapy. During initial phase of therapy, patient whose immune system responds may develop an inflammatory response to indolent or residual opportunistic infections (such as Mycobacterium avium complex, cytomegalovirus, Pneumocystis jiroveci pneumonia, and tuberculosis), which may necessitate further evaluation and treatment.

Patient teaching

• Advise patient to take with a meal or snack. Inform him that he may mix oral powder with nonacidic fluids.
• Tell patient he may take missed dose up to 1 hour before next scheduled dose.

Instruct patient to report depression or suicidal thoughts.
• Tell patient that drug may predispose him to other infections, especially fungal and EENT infections. Advise him to avoid crowds and to wash hands often and thoroughly.
• Tell patient with phenylketonuria (or caregiver) that powder contains phenylalanine.

Tell patient to immediately report new or worsening signs or symptoms.

Advise patient not to use St. John's wort while taking this drug.
• Advise female patient to use reliable barrier contraception.
• Advise female patient not to breastfeed, because breast milk may transfer HIV to infant.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, strength, and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, foods, and herbs mentioned above.


neomycin sulfate

Neo-Fradin, Nivemycin (UK)


Pharmacologic class: Aminoglycoside

Therapeutic class: Anti-infective

Pregnancy risk category D

 

FDABOXED WARNING

Systemic absorption follows oral use and may lead to toxic reactions. Observe patient closely for indications of toxicity. Neurotoxicity (including ototoxicity) and nephrotoxicity have occurred, even at recommended doses. Perform serial, vestibular, and audio-metric tests as well as renal function tests, especially in high-risk patients. Risk of nephrotoxicity and ototoxicity is greater in patients with renal impairment. Ototoxicity may be delayed, and patients developing cochlear damage won't have symptoms during therapy; total or partial deafness may occur long after drug is stopped.

Neuromuscular blockage and respiratory paralysis may follow oral use. Consider these risks, especially to patients receiving anesthetics or neuromuscular blockers (such as tubocurarine, succinylcholine, and decamethonium) and those receiving massive transfusions of citrated anti-coagulated blood. If blockage occurs, calcium salts may reverse these phenomena, but patient may need mechanical respiratory assistance.

Avoid concurrent or sequential systemic, oral, or topical use of other aminoglycosides or neurotoxic drugs, as toxicity may be additive.

Advanced age and dehydration increase risk of toxicity.

Avoid giving drug concurrently with potent diuretics, as some diuretics are ototoxic. Also, I.V. diuretics may enhance neomycin toxicity by altering its blood and tissue levels.

Action

Interferes with bacterial protein synthesis by binding to 30S ribosomal subunit, causing misreading of genetic code. Inaccurate peptide sequence then forms in protein chain, causing bacterial death.

Availability

Ointment: 0.5%

Oral solution: 125 mg/5 ml

Tablets: 500 mg

Indications and dosages

Preoperative intestinal antisepsis

Adults: 1 g P.O. q hour for four doses, then 1 g q 4 hours for 24 hours or 1 g at 19 hours, 18 hours, and 9 hours before surgery

Hepatic encephalopathy

Adults: 4 to 12 g/day P.O. in divided doses

Superficial bacterial infections

Adults: Apply ointment topically one to five times daily.

Contraindications

• Hypersensitivity to drug or other aminoglycosides
• Intestinal obstruction

Precautions

Use cautiously in:
• renal impairment, neuromuscular diseases (such as myasthenia gravis), hearing impairment
• obese patients
• elderly patients
• pregnant or breastfeeding patients
• children under age 18 (safety not established).

Administration

• Give preoperative dose before bowel surgery, after cathartic administration, as ordered.

Adverse reactions

CNS: neuromuscular blockade

EENT: ototoxicity (with prolonged, high-dose use)

GI: nausea, vomiting, diarrhea, malabsorption syndrome

GU: nephrotoxicity (with prolonged, high-dose use)

Other: superinfection

Interactions

Drug-drug.Acyclovir, amphotericin B, cephalosporin, cisplatin, other amino-glycosides, vancomycin: increased risk of ototoxicity and nephrotoxicity

Digoxin: decreased digoxin absorption

Dimenhydrinate: masking of ototoxicity symptoms

Oral anticoagulants: increased anticoagulant effect

Potent loop diuretics: increased risk of ototoxicity

Patient monitoring

• Assess for neuromuscular blockade, ototoxicity, and nephrotoxicity.
• Monitor kidney function tests.

Patient teaching

• Instruct patient to drink plenty of water.
• Tell patient to complete full course of therapy.
• Inform patient that drug may cause muscle weakness.
• Instruct patient to report hearing problems and change in urination pattern.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects neuromuscular status.
• Tell patient he'll undergo frequent blood testing during therapy.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.


neostigmine bromide

Prostigmin



neostigmine methylsulfate

PMS-Neostigmine Methylsulfate, ProstigminNatrecorViramune, Viramune XRCardene, Cardene IV, Cardene SR

Pharmacologic class: Anticholinesterase

Therapeutic class: Muscle stimulant

Pregnancy risk category C

Pharmacologic class: Human B-type natriuretic peptide

Therapeutic class: Vasodilator

Pregnancy risk category C

Pharmacologic class: Nonnucleoside reverse transcriptase inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category C

Pharmacologic class: Calcium channel blocker

Therapeutic class: Antianginal, antihypertensive

Pregnancy risk category C

FDA Box Warning

Drug has caused severe, life-threatening, and in some cases fatal hepatotoxicity, particularly in first 18 weeks. In some cases, patients had nonspecific, prodromal signs or symptoms of hepatitis and progressed to hepatic failure. These events are commonly associated with rash. Women and patients with higher CD4+ cell counts at initiation of therapy are at increased risk. Women with CD4+ cell counts greater than 250/mm3, including pregnant women receiving nevirapine in combination with other antiretrovirals for treatment of HIV-1 infection, are at greatest risk. However, hepatotoxicity associated with nevirapine use can occur in both men and women, and at any time during treatment. Hepatic failure has also been reported in patients without HIV taking nevirapine for postexposure prophylaxis (PEP). Use of nevirapine for occupational and nonoccupational PEP is contraindicated. Patients must discontinue drug and seek immediate medical help if they develop hepatitis signs or symptoms or have increased transaminase levels along with rash or other systemic symptoms.

Severe, life-threatening skin reactions (including fatal cases) have occurred; these have included Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions. Patients who develop signs or symptoms of severe skin reactions or hypersensitivity reactions must discontinue drug and seek immediate medical help.

Monitor patients intensively during first 18 weeks of therapy. Be especially vigilant during first 6 weeks. Don't restart drug in patient who has had clinical hepatitis or transaminase elevations combined with rash or other systemic symptoms, or after severe rash, or hypersensitivity reaction.

Action

Inhibits enzyme acetylcholinesterase, leading to increased acetylcholine concentration at synapse and prolonged acetylcholine effects. Exerts direct cholinomimetic effect on skeletal muscle.

Availability

Injection (methylsulfate): 2 mg/ml, 1 mg/ml, 0.5 mg/ml, 0.25 mg/ml

Tablets (bromide): 15 mg

Indications and dosages

Myasthenia gravis

Adults: 15 mg/day P.O.; may increase p.r.n. up to 375 mg/day; average dosage is 150 mg/day. Or 1 ml of 1:2,000 solution (0.5 mg) subcutaneously or I.M. based on response and tolerance.

Postoperative abdominal distention and bladder atony

Adults: 0.5 to 1 mg I.M. or subcutaneously. If given for urinary retention and no response occurs within 1 hour, catheterize patient as ordered and repeat dose q 3 hours for five doses.

Antidote for nondepolarizing neuromuscular blockers

Adults: 0.5 to 2.5 mg I.V.; repeat p.r.n. up to 5 mg. Precede initial dose with 0.6 to 1.2 mg atropine sulfate I.V., as ordered.

Contraindications

• Hypersensitivity to cholinergics or bromide
• Mechanical obstruction of GI or urinary tract
• Peritonitis

Precautions

Use cautiously in:
• asthma, peptic ulcer, bradycardia, arrhythmias, recent coronary occlusion, vagotonia, hyperthyroidism, seizure disorder
• pregnant or breastfeeding patients.

Administration

Before giving, ensure that atropine sulfate is available to treat cholinergic crisis.
• Know that atropine may be combined with usual neostigmine dose to decrease risk of adverse reactions.
• Give oral form 1 hour before or 2 hours after a meal.
• Administer I.V. dose undiluted directly into vein or I.V. line. Give 0.5-mg dose slowly over 1 minute.

Keep resuscitation equipment nearby.

Adverse reactions

CNS: dizziness, headache, drowsiness, asthenia, loss of consciousness

CV: hypotension, tachycardia, bradycardia, atrioventricular (AV) block, cardiac arrest

EENT: vision changes, lacrimation, miosis

GI: nausea, vomiting, diarrhea, abdominal cramping, flatulence, increased peristalsis

GU: urinary frequency

Musculoskeletal: muscle cramps, spasms, and fasciculations; joint pain

Respiratory: dyspnea, bronchospasm, respiratory depression, respiratory arrest, laryngospasm

Skin: rash, urticaria, flushing

Other: anaphylaxis

Interactions

Drug-drug.Aminoglycosides, anticholinergics, atropine, corticosteroids, local and general anesthetics: reversal of anticholinergic effects

Cholinergics: additive toxicity

Kanamycin, neomycin, streptomycin: increased neuromuscular blockade

Succinylcholine: potentiation of neuromuscular blockade, prolonged respiratory depression

Patient monitoring

Monitor vital signs. Assess patient for hypotension, bradycardia or tachycardia, AV block, and evidence of impending cardiac arrest.
• Evaluate respiratory and neurologic status.

Patient teaching

• Instruct patient to take tablets 1 hour before or 2 hours after meals.

Tell patient drug may alter his respiratory and cardiac status. Teach him to recognize and immediately report warning signs.
• Caution patient to avoid driving and other hazardous activities until he knows how drug affects concentration, vision, muscle function, and alertness.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs mentioned above.


nesiritide

Natrecor


Pharmacologic class: Human B-type natriuretic peptide

Therapeutic class: Vasodilator

Pregnancy risk category C

 

Action

Binds to receptors on vascular smooth muscle and endothelial cells, causing smooth muscle relaxation and vasodilation. As a result, systemic and pulmonary pressures decrease and diuresis occurs.

Availability

Injection: 1.5 mg in single-use vials

Indications and dosages

Acutely decompensated heart failure in patients who have dyspnea at rest or with minimal activity

Adults: 2 mcg/kg I.V. bolus, followed by continuous I.V. infusion of 0.01 mcg/kg/minute

Contraindications

• Hypersensitivity to drug or its components
• Systolic pressure below 90 mm Hg
• Primary therapy for cardiogenic shock

Precautions

Use cautiously in:
• restrictive or obstructive cardiomyopathy, constrictive pericarditis, pericardial tamponade, renal dysfunction, hypotension
• pregnant or breastfeeding patients.

Administration

Know that nesiritide is a high-alert drug.
• For I.V. use, prime tubing before connecting to patient. Withdraw bolus and infuse over 60 seconds into I.V. port of tubing. Follow immediately with constant infusion delivering 0.01 mcg/kg/minute.
• Know that drug should be mixed and infused in dextrose 5% in water, normal saline solution, or dextrose in half-normal saline solution.

Don't mix with other drug solutions. Always administer through separate line.
• Know that nesiritide therapy beyond 48 hours has not been studied.

Adverse reactions

CNS: dizziness, headache, insomnia, anxiety

CV: hypotension, angina pectoris, bradycardia, ventricular extrasystole, ventricular tachycardia

GI: nausea, vomiting, abdominal pain

Musculoskeletal: leg cramps, back pain

Respiratory: cough, hemoptysis, apnea

Other: injection site reactions

Interactions

Drug-drug.Angiotensin-converting enzyme inhibitors, nitrates: increased hypotension

Bumetanide, enalaprilat, ethacrynate sodium, furosemide, heparin, hydralazine, insulin: physical and chemical incompatibility with nesiritide

Drug-diagnostic tests.Hematocrit, hemoglobin: decreased values

Patient monitoring

• Monitor vital signs and pulmonary artery wedge pressure continuously during and for several hours after infusion.
• Assess cardiovascular status closely.

Patient teaching

• Tell patient he'll be monitored closely during and for several hours after infusion.
• Inform patient that drug may cause serious adverse effects. Reassure him that he'll receive appropriate interventions to relieve symptoms.
• Instruct patient to report chest pain, dizziness, palpitations, and other uncomfortable symptoms.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs and tests mentioned above.


nevirapine

Viramune, Viramune XR


Pharmacologic class: Nonnucleoside reverse transcriptase inhibitor

Therapeutic class: Antiretroviral

Pregnancy risk category C

 

FDABOXED WARNING

Drug has caused severe, life-threatening, and in some cases fatal hepatotoxicity, particularly in first 18 weeks. In some cases, patients had nonspecific, prodromal signs or symptoms of hepatitis and progressed to hepatic failure. These events are commonly associated with rash. Women and patients with higher CD4+ cell counts at initiation of therapy are at increased risk. Women with CD4+ cell counts greater than 250/mm3, including pregnant women receiving nevirapine in combination with other antiretrovirals for treatment of HIV-1 infection, are at greatest risk. However, hepatotoxicity associated with nevirapine use can occur in both men and women, and at any time during treatment. Hepatic failure has also been reported in patients without HIV taking nevirapine for postexposure prophylaxis (PEP). Use of nevirapine for occupational and nonoccupational PEP is contraindicated. Patients must discontinue drug and seek immediate medical help if they develop hepatitis signs or symptoms or have increased transaminase levels along with rash or other systemic symptoms.

Severe, life-threatening skin reactions (including fatal cases) have occurred; these have included Stevens-Johnson syndrome, toxic epidermal necrolysis, and hypersensitivity reactions. Patients who develop signs or symptoms of severe skin reactions or hypersensitivity reactions must discontinue drug and seek immediate medical help.

Monitor patients intensively during first 18 weeks of therapy. Be especially vigilant during first 6 weeks. Don't restart drug in patient who has had clinical hepatitis or transaminase elevations combined with rash or other systemic symptoms, or after severe rash, or hypersensitivity reaction.

Action

Inhibits human immunodeficiency virus (HIV) nonnucleoside reverse transcriptase by binding directly to reverse transcriptase and blocking RNA-dependent and DNA-dependent polymerase activity

Availability

Oral suspension: 50 mg/5 ml

Tablets: 200 mg

Tablets (extended-release): 400 mg

Indications and dosages

Treatment of HIV-1 infection

Adults: 200 mg P.O. daily for 14 days, then 200 mg (immediate-release) P.O. b.i.d., given in combination with other antiretrovirals; 400 mg (extended-release) P.O. daily after either a 14-day 200-mg lead-in regimen or after switching from a 200-mg b.i.d. regimen.

Children ages 15 days and older: 150 mg/m2 (immediate-release tablet or oral suspension) P.O. once daily for 14 days, followed by 150 mg/m2 b.i.d. thereafter. Total daily dosage shouldn't exceed 400 mg for any patient.

Dosage adjustment

• Chronic hemodialysis

Off-label uses

• Prophylaxis of maternal-fetal HIV transmission

Contraindications

• Hypersensitivity to drug or its components
• Moderate or severe hepatic impairment (Child-Pugh Class B or C, respectively)
• Use as part of occupational and nonoccupational postexposure prophylaxis regimens

Precautions

Use cautiously in:
• impaired renal or hepatic function
• pregnant or breastfeeding patients
• children.

Administration

• Be aware that drug should be given alone for first 14 days to reduce incidence of rash.
• If patient experiences rash during 14-day lead-in period with immediate-release form, don't initiate extended-release form until rash has resolved.
• Don't continue immediate-release lead-in dosing regimen beyond

28 days. If immediate-release dosing is interrupted for more than 7 days, restart recommended dosing, including 14-day lead-in dosing.
• For patients who interrupt extended-release dosing for more than 7 days, restart recommended lead-in dosing with immediate-release form using one 200-mg tablet daily for first 14 days.
• Be aware that drug shouldn't be started in adult females with CD4+ cell counts greater than 250/mm3 or in adult males with CD4+ cell counts greater than 400/mm3 because of serious and life-threatening hepatotoxicity, unless benefit outweighs risk.
• Give with or without food.

Adverse reactions

CNS: paresthesia, headache, malaise, fatigue

GI: nausea, diarrhea, abdominal pain

Hematologic: agranulocytosis

Hepatic: hepatitis, hepatotoxicity, hepatic failure

Musculoskeletal: myalgia, pain

Skin: rash, blistering, toxic epidermal necrolysis, Stevens-Johnson syndrome

Other: fever

Interactions

Drug-drug.Antiarrhythmics, antifungals, calcium channel blockers, cancer chemotherapy, ergot alkaloids, immunosuppressants, motility agents, opiate agonists: possible decreased plasma concentrations of these drugs

Anticoagulants: possible increased or decreased anticoagulant plasma concentrations

Clarithromycin, efavirenz, indinavir, ketoconazole, methadone: decreased activity of these drugs

Ethinyl estradiol, norethindrone: decreased contraceptive plasma levels Fluconazole: increased nevirapine level Lopinavir/ritonavir: decreased lopinavir activity

Nelfinavir: decreased nelfinavir active metabolite, minimum nelfinavir concentration

Rifabutin: increased rifabutin level

Drug-diagnostic tests.Alanine amino-transferase, aspartate aminotransferase, bilirubin, gamma-glutamyltransferase: increased levels

Hemoglobin, neutrophils: decreased levels

Drug-herbs.St. John's wort: decreased nevirapine blood level

Patient monitoring

Check closely for rash (which may be first sign of Stevens-Johnson syndrome), especially during first 6 months of therapy.
• Monitor patient's weight, temperature, and chest X-ray periodically.
• Assess patient's appetite and energy and physical activity levels.
• Monitor liver function tests and CBC with white cell differential.

Patient teaching

• Tell patient he may take with or without food.
• Tell patient or caregiver to shake suspension gently before use and that it's important to take the entire measured dose of suspension by using an oral dosing syringe or dosing cup.
• Tell patient or caregiver that the extended-release tablet must be swallowed whole and must not be chewed, crushed, or divided.
• Instruct patient to take missed dose as soon as he remembers. But if it's almost time for next dose, tell him to skip missed dose. Caution him not to double the dose.
• Inform female patient that hormonal contraceptives, implants, or shots may be ineffective during nevirapine therapy. Urge her to use alternative birth-control method.

Teach patient to recognize and immediately report rash, easy bruising or bleeding, and signs and symptoms of hepatotoxicity.
• Inform patient that nevirapine won't cure HIV or prevent its transmission.
• Caution female not to breastfeed, because breast milk may transfer HIV to infant.
• As appropriate, review all other significant and life-threatening adverse reactions and interactions, especially those related to the drugs, tests, and herbs mentioned above.


nicardipine hydrochloride

Cardene, Cardene IV, Cardene SR


Pharmacologic class: Calcium channel blocker

Therapeutic class: Antianginal, antihypertensive

Pregnancy risk category C

 

Action

Inhibits calcium transport into myocardial and vascular smooth muscle cells, causing cardiac output and myocardial contractions to decrease

Availability

Capsules: 20 mg, 30 mg

Capsules (sustained-release): 30 mg, 45 mg, 60 mg

Injection: 2.5 mg/ml in 10-ml ampules

Indications and dosages

Chronic stable angina, given alone or with beta-adrenergic blockers

Adults: Titrate dosage individually, starting with 20 to 40 mg P.O. (immediate-release) t.i.d. Wait at least 3 days before increasing dosage.

Hypertension, given alone or with other antihypertensives

Adults: Titrate dosage individually, starting with 20 mg P.O. (immediate release) t.i.d. Wait at least 3 days before increasing dosage. Dosage range is 20 to 40 mg P.O. t.i.d. Patient may be switched to sustained-release capsules at nearest equivalent daily dosage of immediate-release capsules, starting with 30 mg P.O. b.i.d. Effective range is 30 to 60 mg/day.

Short-term treatment of hypertension when oral therapy isn't feasible or desirable

Adults: Continuous I.V. infusion of 0.5 mg/hour (equal to 20 mg P.O. q 8 hours), or 1.2 mg/hour (equal to 30 mg P.O. q 8 hours), or 2.2 mg/hour (equal to 40 mg P.O. q 8 hours)

Off-label uses

• Raynaud's disease
• Heart failure
• Migraine

Contraindications

• Hypersensitivity to drug
• Advanced aortic stenosis

Precautions

Use cautiously in:
• hepatic or mild renal impairment
• hypotension, heart failure, significant left ventricular dysfunction
• pheochromocytoma
• pregnant or breastfeeding patients (safety not established)
• children younger than age 18 (safety not established).

Administration

• Give immediate-release capsules without regard to meals; if GI upset occurs, give with meals. Don't give with grapefruit or grapefruit juice.
• Don't open, crush, break, or let patient chew sustained-release capsules. Give with meals, but not with high-fat meals, grapefruit, or grapefruit juice.
• For I.V. use, dilute each 25-mg ampule with 240 ml of compatible I.V. fluid (such as dextrose 5% in water, normal saline solution, dextrose 5% with normal saline solution, or half-normal saline solution) to a concentration of 0.1 mg/ml.

Don't dilute with sodium bicarbonate 5% or lactated Ringer's injection (incompatible).
• Don't mix with furosemide, heparin, or thiopental.

Give by slow I.V. infusion. Titrate dosage to blood pressure response.

Adverse reactions

CNS: dizziness, headache, asthenia, drowsiness, paresthesia

CV: hypotension, peripheral edema, chest pain, increased angina, palpitations, tachycardia

GI: nausea, dyspepsia, dry mouth

Musculoskeletal: myalgia

Skin: flushing

Interactions

Drug-drug.Cimetidine: increased nifedipine blood level

Cyclosporine: increased cyclosporine blood level

Fentanyl anesthesia: increased hypotension

Drug-food.Grapefruit, grapefruit juice: increased drug blood level and effects

High-fat meal (sustained-release form): decreased drug blood level

Drug-herbs.Ephedra (ma huang), yohimbine: antagonism of drug's anti-hypertensive effect

St. John's wort: decreased nifedipine blood level

Drug-behaviors.Alcohol use: additive hypotension, increased drowsiness or dizziness

Patient monitoring

• Assess vital signs and cardiovascular status.
• Monitor fluid intake and output. Assess for signs and symptoms of heart failure.

Patient teaching

• Tell patient he may take immediate-release capsules without regard to meals. If GI upset occurs, advise him to take them with food, but not with grapefruit or grapefruit juice.
• Tell patient not to open, crush, break, or chew sustained-release capsules. Instruct him to take them with meals, but not with high-fat meals, grapefruit, or grapefruit juice.
• Tell patient to monitor blood pressure and report abnormal findings.

Advise patient to immediately report chest pain or blood pressure drop.
• Instruct patient to consult prescriber before drinking alcohol or taking herbs or over-the-counter drugs (especially cold remedies).
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, foods, herbs, and behaviors mentioned above.


nicotine

Prostigmin

(prŏs-tĭg′mĭn)
A trademark for preparations of the drug neostigmine.

Prostigmin

a trademark for a cholinergic (neostigmine bromide).

Prostigmin

A brand name for NEOSTIGMINE.