neostigmine methylsulfate


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Related to neostigmine methylsulfate: myasthenia gravis

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

neostigmine methylsulfate

A preparation of neostigmine used for parenteral administration in treatment of myasthenia gravis.
See also: neostigmine