Alspan

Rx                 ALSPAN

COMPOSITION:

ALSPAN 1 TAB

Each tablet contains

Hyoscine Butylbromide          10mg

DESCRIPTION:

ALSPAN contains Hyoscine Butylbromide, a potent antispasmodic agent. It is a quaternary ammonium compound and a semisynthetic derivative of scopolamine. It is a peripherally acting antimuscarinic, anticholinergic agent used as an abdominal-specific antispasmodic.

ALSPAN is used to treat pain and discomfort caused by abdominal cramps, menstrual cramps, or other spasmodic activity in the digestive system. It is also effective at preventing bladder spasms. It is not an analgesic in the normal sense, since it doesn't 'mask' or 'cover over' the pain, but rather works to prevent painful cramps and spasms from occurring in the first place. The attachment of the butyl-bromide moiety effectively prevents the movement of this drug across the blood–brain barrier, effectively minimising undesirable CNS side-effects associated with scopolamine/hyoscine.

PHARMACOLOGY

PHARMACODYNAMICS

ALSPAN exerts a spasmolytic action on the smooth muscle of the gastrointestinal, biliary and urinary tracts. Peripheral anticholinergic effects result from a ganglion-blocking action within the visceral wall as well as from anti-muscarinic activity. Relaxation of smooth muscle and reduction of gastric and intestinal motility and relaxation of renal pelvis and ureters are its main benefits. As a quaternary ammonium derivative, ALSPAN does not enter the central nervous system. Therefore, anticholinergic side effects at the central nervous system are insignificant.

PHARMACOKINETICS

Absorption:

ALSPAN is highly polar and hence only partially absorbed, oral absorption of Hyoscine butylbromide is found to be 9%±1% and does not readily pass the blood brain barrier or enter the CNS. Nevertheless, despite the briefly measurable low blood levels, ALSPAN and/or its metabolites have been observed at the sites of action because of its high tissue affinity.

Distribution:

Plasma protein binding is 10%.

Metabolism:

Metabolism is reported hepatic.

Excretion:

Renal Excretion accounts for >2% and plasma half life is 8 hr.

Indications:

• Muscle spasm of the gastrointestinal, renal and biliary tracts.
• Spasmodic dysmenorrhoea.

CONTRAINDICATIONS:

• ALSPAN is contraindicated in myasthenia gravis, megacolon and in patients who have demonstrated prior sensitivity to the product.
• Untreated narrow angle glaucoma; tachycardia, hypertrophy of the prostate with urinary retention; and mechanical stenoses of the gastrointestinal tract.

WARNING AND PRECAUTIONS:

• Because of the potential risk of anticholinergic complication, ALSPAN tablets should be administered with caution in patients susceptible to narrow angle glaucoma, intestinal or urinary outlet obstruction and those inclined to tachyarrhythmia.

• Pregnancy and Lactation: Precautions, especially during the first trimester, should be observed. Safety during lactation has not yet been established; however, adverse effects on the newborn have not been reported.

DRUG INTERACTIONS:

Tri-and tetracyclic antidepressants Antipsychotics Atropine-like compounds	Can potentiate the anticholinergic effect.
Antihistamines	Can potentiate the anticholinergic effect.
Quinidine	Can potentiate the anticholinergic effect.
Disopyramide	Can potentiate the anticholinergic effect.
Amantadine	Can potentiate the anticholinergic effect.
MAO inhibitors	May result in intensified anticholinergic side effects. Also, may block detoxification of anticholinergics thus potentiating their action.

                  

• Concomitant treatment with dopamine antagonists such as metoclopramide may result in diminution of the effects of both drugs on the gastrointestinal tract.
• The tachycardic effects of beta-adrenergic agents may be enhanced.
• Atropine, an anticholinergic (Parasympatholytic) completely blocks the muscarinic receptors in peripheral tissues. Atropine due to its vegal activity has thus benefit in Bradycardia, and in reducing the heart block. While reducing glandular secretion, Atropine also helps in relaxation of smooth muscle Bronchi and guts. Thus antispasmodic activity is limited.
• The mode of action of Dicyclomine is similar to that of Hyoscine butylbromide. Dicyclomine, a synthetic antimuscarinic- blocks cholinergic transmission at parasympathetic postaganglionic nerve endings innervating to smooth muscle, causeing it to relax.

ADVERSE EFFECTS:

• Anticholinergic side effects including xerostomia, dyshidrosis, tachycardia, and urinary retention may occur but are generally mild and self-limited.
• Very rarely hypersensitivity reaction particularly skin reaction and, in extremely rare cases, dyspnea have been reported.

DOSAGE AND ADMINISTRATION:

The dosage range is 1-4 tablets (10-40 mg) per day depending upon the severity of the condition. The tablets should be swallowed whole with adequate fluid.

OVERDOSAGE:

Serious signs of poisoning following acute overdosage have not been observed in man.  In the case of overdosage, anticholinergic effects such as urinary retention, dry mouth, reddening of the skin, tachycardia, inhibition of gastro-intestinal motility and transient visual disturbances may occur, and Cheynes-Stokes respiration has been reported.

STORAGE:
Store in a cool and dry place