Propantheline Bromide; Uses, Dosage, Side Effects, Interactions

Propantheline bromide is a muscarinic antagonist used as an antispasmodic, in rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking.

Propantheline Bromide is the bromide salt form of propantheline, a quaternary ammonium compound structurally related to belladonna alkaloids. Propantheline bromide competitively antagonizes acetylcholine activity mediated by muscarinic receptors at neuroeffector sites on smooth muscle and exocrine gland cells. An aspartic acid residue present in the N-terminal portion of the third trans-membrane helix of the muscarinic receptor is believed to form an ionic bond with the tertiary or quaternary nitrogen of the antagonist. Antagonism leads to a reduction of exocrine glands secretions and to relax bronchial muscle and reduce tone and motility of intestinal smooth muscle.

Propantheline bromide (INN) is a muscarinic antagonist used as an antispasmodic, for the treatment of excessive sweating (hyperhidrosis), cramps or spasms of the stomach, intestines (gut) or bladder, and involuntary urination (enuresis)rhinitis, in urinary incontinence, and in the treatment of ulcers. At high doses it has nicotinic effects resulting in neuromuscular blocking It can also be used to control the symptoms of irritable bowel syndrome and similar conditions. This agent can also be used for patients who experience intense GI symptoms while tapering off of TCAs.

Mechanism of Action of Propantheline Bromide

Propantheline is one of a group of antispasmodic medications which work by blocking the action of the chemical messenger acetylcholine, which is produced by nerve cells, to muscarinic receptors present in various smooth muscular tissues, in places such as the gut, bladder and eye. Normally, the binding of acetylcholine induces involuntary smooth muscular contractions.

Indications of Propantheline Bromide

• Hyperhidrosis
• Adult enuresis
• Peptic Ulcers
• It is used to relieve cramps in the stomach, intestine and genito-urinary tract, and other conditions characterised by spasm of the smooth muscles found in these areas.
• In general this drug is used to treat spasms in the gastrointestinal tract. Other uses include the prevention of involuntary release of urine (in adults) by relaxing the muscles which cause this problem. It is also used to prevent excessive sweating (hyperhidrosis).
• Benefits of being on this drug include reducing spasms in the gastrointestinal tract, as well as preventing involuntary urine release and excessive sweating.
• Adjunctive in GI disorders characterised by smooth muscle spasm
• Relaxing the smooth muscle in the bladder prevents the involuntary spasms that can allow leakage of urine from the bladder in the condition known as enuresis
• Treatment of excessive sweating because acetylcholine block also reduces secretions such as sweat and tears.

Contra Indications of Propantheline Bromide

• Overactive thyroid gland
• Myasthenia gravis
• Closed angle glaucoma
• High blood pressure
• Coronary artery disease
• Chronic heart failure
• Chronic lung disease
• A change in saliva secretion
• Failure of esophageal sphincter to relax
• Inflammation of esophagus from backflow of stomach acid
• Stomach ulcer
• Narrowing of opening between stomach and small intestine
• Hiatal hernia
• Ulcerated colon
• Severe ulcerative colitis
• Toxic megacolon
• Paralysis of the intestines
• Stomach or intestine blockage
• Atony of colon
• Liver problems
• kidney disease with a reduction in kidney function
• Blockage of the urinary bladder
• Urinary tract blockage
• Enlarged prostate
• Down syndrome
• Drowsiness
• Fast heartbeat
• Cannot empty bladder
• Toxin from Microorganisms causing diarrhea
• Bleeding causing blood pressure or heart problems
• Dysreflexia

Dosages of Propantheline Bromide

Strengths: 15 mg; 7.5 mg

Peptic Ulcer

Initial dose:

• 15 mg orally taken 30 minutes before each meal and 30 mg orally at bedtime (a total of 75 mg/day)

Peptic Ulcer

Initial dose:

• 7.5 mg orally 3 times a day, taken 30 minutes before each meal

Side Effects of Propantheline Bromide

The most common

• Constipation.
• Blurred vision.
• Difficulty passing urine (urinary retention).
• Dry mouth.
• Difficulty in breathing
• Headache
• Weight gain
• Nausea
• Upset stomach
• Decreased appetite
• Diarrhea

More common

• Sweating
• Blurred vision
• Dizziness.
• slower heart rate
• change in sex drive or performance
• diarrhea
• dry eyes
• hair loss
• nausea
• weakness or tiredness

Common

• Cough producing mucus
• difficulty with breathing
• tightness in the chest
• Abdominal or stomach pain and tenderness
• blistering, peeling, or loosening of the skin
• Anxiety
• dry mouth
• irritability
• sleepiness or unusual drowsiness
• trouble sleeping
• Decreased appetite
• Dilated pupils, with increased sensitivity to light.
• Increased pressure within the eye.
• Heat stroke (see warning section above).
• Changes in heart rate.
• Awareness of your heart beat (heart palpitations).
• Abnormal heart beats (arrhythmias).
• Confusion in elderly people.

Drug Interactions of Propantheline Bromide

Propantheline bromide may interact with following drugs, supplement & may change the efficacy of drugs

• Dilated pupils, with increased sensitivity to light.
• antihistamines (e.g., diphenhydramine, meclizine),
• antispasmodics (e.g., dicyclomine), belladonna alkaloids (e.g., scopolamine, atropine),
• diphenhydramine, hydroxyzine, loratadine)
• antipsychotics (e.g., chlorpromazine, clozapine, haloperidol, olanzapine, quetiapine, risperidone)
• antiseizure medications (e.g., clobazam,  phenobarbital, phenytoin,   valproic acid, zonisamide)
• aripiprazole
• “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
• baclofen
• barbiturates (e.g., butalbital, pentobarbital, phenobarbital)
• benzodiazepines (e.g., alprazolam, diazepam, lorazepam)
• domperidone
• famotidine
• gabapentin
• ipratropium
• ketotifen
• levodopa
• macrolide antibiotics (e.g., azithromycin, clarithromycin, erythromycin)
• magnesium sulfate
• methylphenidate
• mirtazapine
• monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, rasagiline, selegiline, tranylcypromine)
• muscle relaxants (e.g., cyclobenzaprine, methocarbamol, orphenadrine)
• orphenadrine
• quinolone antibiotics (e.g., levofloxacin, norfloxacin, moxifloxacin)
• selective serotonin reuptake inhibitors (SSRIs; e.g., paroxetine, fluoxetine, citalopram)
• serotonin antagonists (anti-emetic medications; e.g., granisetron, ondansetron)
• sotalol
• tapentadol
• thiazide diuretics (water pills; e.g., hydrochlorothiazide, indapamide, )
• thioridazine
• tolterodine
• tramadol
• trimethoprim
• tricyclic antidepressants (e.g., amitriptyline, clomipramine, desipramine, trimipramine)
• “triptan” migraine medications (e.g., eletriptan, sumatriptan)
• tryptophan
• tyrosine kinase inhibitors (e.g., dasatinib, imatinib, nilotinib, sunitinib)
• muscle relaxants, narcotic pain relievers (e.g., meperidine, codeine),
• psychiatric medicines (e.g., chlorpromazine, risperidone, trazodone).

Pregnancy and Lactation of Propantheline Bromide

FDA Pregnancy Category C

Pregnancy