SUPP-notes2009 - PHCY 6100 SUPPOSITORIES INSERTS...

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PHCY 6100 SUPPOSITORIES & INSERTS PHCY 6100-Teixeira 1 SUPPOSITORIES (supponere = place “under” the body) i) Def. Solid dosage forms used to administer medications through the rectum, vagina or urethra, where they melt or soften and dissolve to exert localized or systemic effect. ii) Advantages of suppositories Avoid gastric pH and enzymes Avoid irritation of stomach Bypass liver = avoid first pass effect (partially) Useful for patients unwilling or unable to swallow Useful for patients that are vomiting Alternative route if parenteral route is unsuitable Fast acting iii) Some regularly compounded suppositories: For severe nausea & vomiting: metoclopramide, haloperidol, dexamethasone, diphenhydramine and benztropine Long-term prophylactic treatment of asthma: salbutamol For chronic pain: prolonged-release morphine alkaloid iv) Factors affecting drug absorption from suppositories For rectal suppositories: (A) COLONIC CONTENT: empty rectum will allow maximal absorption; diarrhea, rectal tumors, dehydration may affect rate and degree of absorption. (B) CIRCULATION ROUTE: lower hemorrhoidal veins and lymphatics surrounding the colon receive most of the absorbed drug and initiate its circulation, bypassing the liver. (C) PH and BUFFERING CAPACITY: rectal fluid pH is ~ neutral, so no buffering capacity and no chemical changes of drug happen at the site. For all suppositories: (A) LIPID-WATER SOLUBILITY: partition coefficient of drug is important for decision on suppository base to be used. (B) PARTICLE SIZE: smaller have faster dissolution and absorption. (C) NATURE OF THE BASE: a good supp. base must i. Melt at body temperature /soften and dissolve in body fluids; ii. Be able to release the drug for absorption (principle of opposite characteristics: water- soluble drugs in oil-soluble base and vice-versa). iii. Be non-irritating to mucous membranes (exception if for laxative purposes). RECTAL SUPPOSITORIES a) Cylindrical, torpedo, bullet or little finger. b) Adult: ~ 1 ½inch long; ~2g (cocoa butter base) c) Pediatric: half weight and size. d) Application: with fingers. e) Uses
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PHCY 6100 SUPPOSITORIES & INSERTS PHCY 6100-Teixeira 2 i) Local Effect : relief of constipation and hemorrhoids or anorectal discomforts. Ex: glycerin suppositories: used as cathartic (=laxative) ii) Systemic Effect : for administration of antiemetics, tranquilizers, anti-inflammatories, treatment of asthma, etc. Absorption occurs through the mucous membranes of the rectum into the hemorrhoidal veins and lymphatic circulation. f) Patient counseling Handwashing Packaging material Insertion depends on shape Half suppository If suppository is stored in refrigerator, allow to warm at room temperature or rotate between the palms of hands for a while.
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