Pamine

Generic Name: Methscopolamine Bromide
Class: Antimuscarinics/Antispasmodics
VA Class: AU350
Chemical Name: [7(S) - 1α,2β,4β,5α,7β] - 7 - (3 - hydroxy - 1 - oxo - 2 - phenylpropoxy) - 9,9 - dimethyl - 3 - oxa - 9 - azoniatricyclo[3,3,1,02,4] nonane bromide
Molecular Formula: C₁₈H₂₄BrNO₄
CAS Number: 155-41-9

Introduction

Antimuscarinic; semisynthetic quaternary ammonium derivative of scopolamine.^{a b d}

Uses for Pamine

Peptic Ulcer Disease

Adjunctive therapy in the treatment of peptic ulcer disease;^{a b c d} however, no conclusive data that antimuscarinics aid in the healing, decrease the rate of recurrence, or prevent complications of peptic ulcers.^{a b c d}

With the advent of more effective therapies for the treatment of peptic ulcer disease, antimuscarinics have only limited usefulness in this condition. ^{a c}

Pamine Dosage and Administration

Administration

Administer orally 30 minutes before meals and at bedtime.^{a b d}

Dosage

Available as methscopolamine bromide; dosage expressed in terms of the salt.^{a b}

As with other antimuscarinics, may require a higher than recommended dosage for therapeutic effect.^c Titrate dosage carefully according to individual requirements and response.^{a d} Administer lowest effective dosage to minimize risk and occurrence of adverse effects.^{a c d}

Pediatric Patients

Peptic Ulcer Disease†

Oral

0.2 mg/kg or 6 mg/m² daily in 4 equally divided doses has been recommended by some clinicians.^a (See Pediatric Use under Cautions.)

Adults

Peptic Ulcer Disease

Oral

Initially, 2.5 mg 3 times daily before meals and 2.5–5 mg at bedtime.^{a b d} Manufacturer states that an initial total daily dosage of 12.5 mg is effective in most patients.^{a b d}

Patients with severe symptoms (e.g., abdominal pain, cramping): Initially, 5 mg 3 times daily before meals and once at bedtime (total daily dosage of 20 mg).^{a b d} If patient experiences adverse effects, reduce dosage; if symptoms are unrelieved and there are no adverse effects, may increase dosage.^{b d} Some patients may tolerate a total daily dosage up to 30 mg.^{a b d}

Patients who experience severe adverse effects without appreciable relief of symptoms should be considered unsuitable candidates for continued therapy and likely will be intolerant of other antimuscarinics.^{b d} If methscopolamine is used in patients with a history of increased susceptibility to adverse effects from antimuscarinics, initiate drug at a low dosage.^{a b d}

Special Populations

No special population dosage recommendations at this time.^{a b d}

Cautions for Pamine

Contraindications

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  Glaucoma (to avoid mydriasis).^{b c d}

  
  


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  Obstructive uropathy (e.g., bladder neck obstruction caused by prostatic hypertrophy).^{b c d}

  
  


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  Obstructive GI disease (e.g., pyloroduodenal stenosis, paralytic ileus).^{b c d}

  
  


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  Intestinal atony (especially in geriatric and debilitated patients).^{b c d}

  
  


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  Unstable cardiovascular status in acute hemorrhage.^{b c d}

  
  


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  Severe ulcerative colitis or toxic megacolon complicating ulcerative colitis.^{b c d}

  
  


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  Myasthenia gravis.^{b c d}

  
  


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  Known hypersensitivity to methscopolamine or to similar drugs.^{b c d}

  
  

Warnings/Precautions

Warnings

Thermoregulatory Effects

High environmental temperatures may result in heat prostration (e.g., fever, heat stroke) due to decreased sweating.^{b c d}

Diarrhea

May be an early sign of incomplete intestinal obstruction, especially in patients with ileostomy or colostomy.^{b c d} Do not use in such patients; use would be inappropriate and possibly harmful.^{b d}

CNS Effects

Risk of drowsiness or blurred vision.^{b c d} Performance of activities requiring mental alertness (e.g., operating machinery, driving a motor vehicle, performing hazardous work) may be impaired.^{b c d} (See Advice to Patients.)

Overdosage

A curare-like action may occur (i.e., neuromuscular blockade leading to muscular weakness and possible paralysis).^{b d}

Sensitivity Reactions

Hypersensitivity Reactions

Severe allergic reactions and drug idiosyncrasies including anaphylaxis have been reported.^{b d}

General Precautions

GI Effects

Caution in patients with gastric ulcer because of delayed gastric emptying and possible antral stasis.^c

Caution in patients with ulcerative colitis; large doses may suppress intestinal motility, resulting in paralytic ileus and toxic megacolon.^{b c d}

Caution in patients with known or suspected GI infections (e.g., Clostridium difficile-associated diarrhea and colitis, shigellosis, dysentery).^c

Concomitant Illnesses

Use with caution in patients with hyperthyroidism, autonomic neuropathy, CHD, CHF, tachyarrhythmia, hypertension, or prostatic hypertrophy.^{b d}

Laboratory Monitoring

Perform radiography (contrast examination of upper GI tract) or endoscopy to ensure ulcer healing during therapy.^{b d}

Perform periodic hematocrit and hemoglobin tests and test for occult blood in stool during therapy to rule out bleeding from the ulcer.^{b d}

Specific Populations

Pregnancy

Category C.^{b d}

Lactation

Not known whether methscopolamine is distributed into human milk.^{b d} Caution if used in nursing women.^{b d}

May suppress lactation.^{b c d}

Pediatric Use

Safety and efficacy not established.^{b c d}

Geriatric Use

Use with caution.^{b c d}

Hepatic Impairment

Use with caution in patients with hepatic disease.^{b c d}

Renal Impairment

Use with caution in patients with renal disease.^{b c d}

Common Adverse Effects

Xerostomia,^b decreased sweating,^b adverse ocular effects (e.g., blurred vision, mydriasis, cycloplegia, increased ocular tension).^{b c d}

Interactions for Pamine

Drugs with Anticholinergic Effects

Additive adverse effects resulting from cholinergic blockade (e.g., xerostomia, blurred vision, constipation).^c Advise of possibility of increased anticholinergic effects.^c

Orally Administered Drugs

Potential pharmacokinetic interaction (altered GI absorption of various drugs).^c Antimuscarinics may inhibit GI motility, delay gastric emptying, and prolong GI transit time.^c

Specific Drugs

Drug	Interaction	Comments
Amantadine	Possible additive adverse anticholinergic effectsc	Inform patient of possibilityc
Antacids	Possible decreased absorption of methscopolamineb c d	Administer methscopolamine at least 1 hour before antacidsc
Antiarrhythmic agents (e.g., disopyramide, procainamide, quinidine)	Possible additive adverse anticholinergic effectsc	Inform patient of possibilityc
Anticholinergic agents	Risk of additive adverse anticholinergic effectsc	Inform patient of riskc
Antidepressants, tricyclic	Possible additive adverse anticholinergic effectsb c d	Inform patient of possibilityc
Antihistamines	Possible additive adverse anticholinergic effectsc	Inform patient of possibilityc
Antiparkinsonian agents	Possible additive adverse anticholinergic effectsc	Inform patient of possibilityc
Corticosteroids	Possible increased IOPc
Ketoconazole	Possible decreased ketoconazole absorptionc	Administer antimuscarinic ≥2 hours after ketoconazolec
Levodopa	Possible increased gastric levodopa metabolism, resulting in decreased levodopa absorptionc	Possible levodopa toxicity if antimuscarinic is discontinued without a concomitant reduction in levodopa dosagec
Meperidine	Possible additive adverse anticholinergic effectsc	Inform patient of possibilityc
Phenothiazines	Possible additive adverse anticholinergic effectsb c d	Inform patient of possibilityc
Potassium chloride	Antimuscarinics may slow GI transit, increasing risk of potassium chloride GI mucosal toxicityc	Administer concomitantly with caution (especially with wax matrix potassium chloride preparations)c
Skeletal muscle relaxants	Possible additive adverse anticholinergic effectsc	Inform patient of possibilityc

Pamine Pharmacokinetics

Absorption

Bioavailability

Incompletely absorbed from the GI tract because completely ionized.^{a b d}

Onset

Following oral administration, drug effects occur in about 1 hour.^{b d}

Duration

Effects persist 4–6 hours after oral administration.^{b d}

Distribution

Extent

Quaternary ammonium antimuscarinics are completely ionized and possess poor lipid solubility; do not readily cross blood-brain barrier or penetrate the CNS or eye.^{a b c d}

Not known whether methscopolamine crosses the placenta or is distributed into human milk.^{b c d}

Elimination

Elimination Route

Principally in urine and bile (as unchanged drug and metabolites) and in feces (as unabsorbed drug).^{a b d}

Stability

Storage

Oral

Tablets

Tight containers at 15–30°C.^{a b}

ActionsActions

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  Competitively inhibits acetylcholine or other cholinergic stimuli at autonomic effectors innervated by postganglionic cholinergic nerves and, to a lesser extent, on smooth muscles that lack cholinergic innervation.^c

  
  


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  At usual doses, antimuscarinics principally antagonize cholinergic stimuli at muscarinic receptors and have little or no effect on cholinergic stimuli at nicotinic receptors. ^c

  
  


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  Antimuscarinics also have been referred to as anticholinergics (cholinergic blocking agents), but this term is appropriate only when it describes the antagonism of cholinergic stimuli at any cholinergic receptor, whether muscarinic or nicotinic.^c

  
  


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  Antimuscarinics also have been referred to as parasympatholytics since the antagonized functions principally are under the parasympathetic division of the nervous system.^c

  
  


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  Methscopolamine reduces volume and total acid content of gastric secretions.^{b d}

  
  


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  Inhibits GI motility and salivary excretion.^{b d}

  
  


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  Dilates the pupil and inhibits accommodation.^{b d}

  
  

Advice to Patients

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  Potential for hyperthermia and heat prostration; avoid exposure to high environmental temperature and use with caution when febrile.^{b c d}

  
  


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  Risk of drowsiness or blurred vision; exercise caution when performing activities requiring mental alertness (e.g., driving a motor vehicle, operating machinery) or when performing other hazardous work.^{b d}

  
  


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  Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.^{b d}

  
  


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  Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.^{b d}

  
  


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  Importance of informing patients of other important precautionary information.^{b d} (See Cautions.)

  
  

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

* available from one or more manufacturer, distributor, and/or repackager by generic (nonproprietary) name

Methscopolamine Bromide

Routes	Dosage Forms	Strengths	Brand Names	Manufacturer
Oral	Tablets	2.5 mg*	Methscopolamine Bromide Tablets	Boca
			Pamine	Kenwood
		5 mg*	Methscopolamine Bromide Tablets	Boca
			Pamine Forte	Kenwood

Disclaimer

This report on medications is for your information only, and is not considered individual patient advice. Because of the changing nature of drug information, please consult your physician or pharmacist about specific clinical use.

The American Society of Health-System Pharmacists, Inc. and Drugs.com represent that the information provided hereunder was formulated with a reasonable standard of care, and in conformity with professional standards in the field. The American Society of Health-System Pharmacists, Inc. and Drugs.com make no representations or warranties, express or implied, including, but not limited to, any implied warranty of merchantability and/or fitness for a particular purpose, with respect to such information and specifically disclaims all such warranties. Users are advised that decisions regarding drug therapy are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and the information is provided for informational purposes only. The entire monograph for a drug should be reviewed for a thorough understanding of the drug's actions, uses and side effects. The American Society of Health-System Pharmacists, Inc. and Drugs.com do not endorse or recommend the use of any drug. The information is not a substitute for medical care.

AHFS Drug Information. © Copyright, 1959-2011, Selected Revisions June 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.

† Use is not currently included in the labeling approved by the US Food and Drug Administration.

References

a. AHFS Drug Information 2008. McEvoy GK, ed. Methscopolamine. Bethesda, MD: American Society of Health-System Pharmacists; 2008:1319.

b. Kenwood Therapeutics. Pamine Forte and Pamine (methscopolamine bromide) prescribing information. Fairfield, NJ; 2005 May.

c. AHFS Drug Information 2008. McEvoy GK, ed. Antimuscarinics/Antispasmodics General Statement. Bethesda, MD: American Society of Health-System Pharmacists; 2008:1293-1300.

d. Boca Pharmacal, Inc. Methscopolamine bromide tablets prescribing information. Coral Springs, FL; 2006 Jan.

More Pamine resources

• Pamine Side Effects (in more detail)
• Pamine Dosage
• Pamine Use in Pregnancy & Breastfeeding
• Drug Images
• Pamine Drug Interactions
• Pamine Support Group
• 2 Reviews for Pamine - Add your own review/rating

• Pamine Prescribing Information (FDA)


• Pamine Concise Consumer Information (Cerner Multum)


• Pamine MedFacts Consumer Leaflet (Wolters Kluwer)


• Methscopolamine Prescribing Information (FDA)

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