scopolamine hydrobromide

scopolamine hydrobromide (hyoscine hydrobromide)

Buscopan (UK), Kwells (UK)

Pharmacologic class: Antimuscarinic, belladonna alkaloid

Therapeutic class: Antiemetic, antivertigo agent, anticholinergic

Pregnancy risk category C

Action

Acts as competitive inhibitor at postganglionic muscarinic receptor sites of parasympathetic nervous system and on smooth muscles that respond to acetylcholine but lack cholinergic innervation. May block cholinergic transmission from vestibular nuclei to higher CNS centers and from reticular formation to vomiting center.

Availability

Injection: 1 mg/ml in 1-ml vials, 0.4 mg/ml in 0.5-ml ampules and 1-ml vials, 0.86 mg/ml in 0.5-ml ampules

Transdermal system (Transderm-Scop): 1.5 mg/patch (releases 0.5 mg scopolamine over 3 days)

Indications and dosages

Preanesthetic sedation and obstetric amnesia

Adults: 0.3 to 0.6 mg I.M., I.V., or subcutaneously 45 to 60 minutes before anesthesia, usually given with analgesics

Postoperative nausea and vomiting

Adults: One transdermal patch placed behind ear on evening before surgery and kept in place for 24 hours after surgery. For cesarean section, one transdermal patch placed behind ear 1 hour before surgery.

Motion sickness

Adults: One transdermal patch placed behind ear 4 hours before anticipated need, replaced q 3 days if needed

Contraindications

• Hypersensitivity to scopolamine, other belladonna alkaloids, or barbiturates
• Hypersensitivity to bromides (injection only)
• Angle-closure glaucoma
• Acute hemorrhage
• Myasthenia gravis
• Obstructive uropathy (including prostatic hypertrophy)
• Obstructive GI disease (including paralytic ileus and intestinal atony)
• Reflux esophagitis
• Ulcerative colitis or toxic megacolon
• Hepatic or renal impairment
• Chronic lung disease (with repeated doses)

Precautions

Use cautiously in:
• suspected intestinal obstruction; pulmonary or cardiac disease; tachyarrhythmia or tachycardia; open-angle glaucoma; autonomic neuropathy; hypertension; hyperthyroidism; ileostomy or colostomy
• history of seizures or psychosis
• elderly patients
• pregnant or breastfeeding patients (safety not established)
• children.

Administration

• For I.V. use, give by direct injection at prescribed rate after diluting with sterile water.
• After removing protective strip from transdermal patch, avoid finger contact with exposed adhesive layer to prevent contamination.

Adverse reactions

CNS: drowsiness, dizziness, confusion, restlessness, fatigue

CV: tachycardia, palpitations, hypotension, transient heart rate changes

EENT: blurred vision, mydriasis, photophobia, conjunctivitis

GI: constipation, dry mouth

GU: urinary hesitancy or retention

Skin: decreased sweating, rash

Interactions

Drug-drug.Antidepressants, antihistamines, disopyramide, quinidine: additive anticholinergic effects

Antidepressants, antihistamines, opioid analgesics, sedative-hypnotics: additive CNS depression

Oral drugs: altered absorption of these drugs

Wax-matrix potassium tablets: increased GI mucosal lesions

Drug-herbs.Angel's trumpet, jimsonweed, scopolia: increased anticholinergic effects

Drug-behaviors.Alcohol use: increased CNS depression

Patient monitoring

• Assess vital signs and neurologic, cardiovascular, and respiratory status.
• Monitor patient for urinary hesitancy or retention.

Patient teaching

• Tell patient transdermal patch is most effective if applied to dry skin behind ear 4 hours before traveling.
• Caution patient to avoid touching exposed adhesive layer of transdermal patch.
• Advise patient to wash and dry hands thoroughly before and after applying patch.
• If patch becomes dislodged, instruct patient to remove it and apply new patch on a different site behind ear.
• Tell patient that using patch for more than 72 hours may cause withdrawal symptoms (headache, nausea, vomiting, dizziness). Advise him to limit use when feasible.
• Inform patient that his eyes may be markedly sensitive to light during patch use. Instruct him to wear sunglasses and use other measures to guard eyes from light.
• Caution patient to avoid alcohol because it may increase CNS depression.
• As appropriate, review all other significant adverse reactions and interactions, especially those related to the drugs, herbs, and behaviors mentioned above.

scopolamine hydrobromide

(sko-pol'a-men hi?dro-bro'mi)
The hydrobromide of alkaloids obtained from plants of the nightshade family. Synonym: hyoscine hydrobromide

Action/Uses

The drug is used to prevent vertigo and motion sickness, to sedate patients, and to produce amnesia in anesthesia. Its adverse effects include confusion, hallucinations, and unwanted memory loss, which may be especially prominent in elderly patients.

transdermal scopolamine

A method of delivering scopolamine by applying a patch containing the drug to the skin. The medicine is slowly absorbed over a period of several days. It is esp. useful in treating vertigo and motion sickness. In the latter condition, the medicine is effective if applied several hours before the individual is exposed to the motion.

hyoscine hydrobromide

An antimuscarinic (or parasympatholytic) drug with actions similar to those of atropine (i.e. mydriasis and cycloplegia) but of shorter duration. It is used in the measurement of refraction of children and in the treatment of keratitis, anterior uveitis and in cases of burns to the anterior segment of the eye to prevent posterior synechia, as well as to reduce the pain secondary to iridociliary spasm. Syn. scopolamine hydrobromide.
References in periodicals archive ?
Drugs and Drugs, Vitamin supplements, scopolamine hydrobromide, Alteplase
Scopolamine hydrobromide (Sigma, Germany) was dissolved in an isotonic solution (0.
SANTIAGO, CHILE -- Treatment with scopolamine hydrobromide blocks muscarinic cholinergic receptors and produces a rapid, robust antidepressant response in depressed patients with unipolar or bipolar depression, Maura L.
In addition to intranasal morphine for treatment of moderate-to-severe pain, including breakthrough pain, Nastech has several products in clinical development including intranasal scopolamine hydrobromide for the prevention and treatment of motion sickness, intranasal apomorphine for the treatment of sexual dysfunction, and intranasal butorphanol for the treatment of acute migraine pain.
The Scientific Research Division Laboratory of the New York City Police Department and the New York County Medical Examiner's Office identified scopolamine hydrobromide, lorazepam, and atrophine as three of the more commonly used knock-out substances.
The Company utilizes its proprietary STA-T(TM) process to administer intranasally for systemic effect a portfolio of drugs for indications that are mediated through the central nervous system, including scopolamine hydrobromide for the prevention and treatment of motion sickness, apomorphine hydrochloride for the treatment of sexual dysfunction, morphine for treatment of moderate-to-severe pain, including breakthrough pain, and butorphanol tartrate for treatment of migraine pain.
Nasdaq: NSTK) announced today that it has met with the FDA concerning its NDA for intranasal scopolamine hydrobromide, which is indicated for the prevention and treatment of motion sickness.
Scopolamine hydrobromide (Sigma-Aldrich, USA), diazepam (Ranbaxy, India), 5,5-dithiobis-2-nitrobenzoic acid (DTNB), acetylcholine iodide, eserine salicylate, sodium dihydrogen phosphate, disodium hydrogen phosphate (Hi Media, India), piracetam (UCB India Ltd.
3 million, a decrease of $661,000 from a year ago, and reflects, primarily, completion of Phase III clinical trials for the company's motion sickness product, intranasal scopolamine hydrobromide.
Moreover, the enhancement of oxotremorine-induced tremors by Ninjin-yoei-to (1000 mg/kg) and Polygalae radix (100 mg/kg) was completely antagonized by pretreatment of scopolamine hydrobromide (0.
In addition to intranasal apomorphine for the treatment of sexual dysfunction, the company is developing intranasal scopolamine hydrobromide for the prevention and treatment of motion sickness and intranasal morphine for the treatment of moderate-to-severe-pain.
Separately, the company reported that the United States Food and Drug Administration (FDA) declined acceptance of its New Drug Application (NDA), submitted in December 1999, for the motion sickness product, intranasal scopolamine hydrobromide.