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What is a primary advantage of using suppositories for drug administration?
Suppositories can be used rectally, vaginally, and orally.
False
Name one disadvantage of using suppositories.
Patient acceptability issues
Glycerin suppositories promote laxation by local irritation of the ______.
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Match the suppository type with its primary use:
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Which of the following is NOT a common use for rectal suppositories?
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Suppositories are suitable for patients suffering from diarrhea.
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What is one way that suppositories can benefit unconscious patients?
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Which of the following is NOT an example of a drug administered rectally for systemic effects?
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Drugs absorbed rectally pass through the portal circulation before entering general circulation.
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What is the neutral pH range of rectal fluids?
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A drug's concentration in the intestinal lumen above a certain amount does not affect the rate of __________.
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Match the following drugs with their respective therapeutic effects:
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What is a key factor that affects the absorption of drugs from rectal suppositories?
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The larger the particle size of a dispersed drug, the better it dissolves and absorbs.
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Which drug is used in rectal suppositories specifically for tranquilization?
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Which property is NOT desired in an ideal suppository base?
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The lipid–water partition coefficient of a drug is significant for anticipating drug release from the suppository base.
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What happens if a suppository base irritates the rectal mucous membranes?
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A lipophilic drug in a suppository base has a tendency to escape to the surrounding _______ fluids.
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Match the following properties with their descriptions regarding the ideal suppository base:
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What characteristic of a suppository base aids in drug release?
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Long acting suppositories are designed to release their drug rapidly for immediate action.
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What is an example of a material used in slow release suppositories?
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Study Notes
Suppositories: Solid Dosage Forms
- Suppositories are solid dosage forms inserted into body cavities (rectum, vagina, urethra)
- They melt, soften, or dissolve, releasing medication for local or systemic effects.
Advantages of Suppositories
- Local effect: Directly targets rectal mucosa.
- Systemic absorption: Bypasses first-pass metabolism, leading to higher bioavailability.
- Drug stability: Protects from gastrointestinal degradation.
- Unconscious patients: Can be administered safely.
- Swallowing difficulties: Useful for infants or elderly individuals.
- Postoperative patients: Alternative to oral administration when swallowing is compromised.
- Nausea & vomiting: Effective when oral medication is not tolerated.
- Bowel evacuation: Promotes defecation.
Disadvantages of Suppositories
- Patient acceptance: Might be uncomfortable for some patients.
- Dosage variation: Rectal dose may differ from oral dose.
- Diarrhea: Not suitable for patients with diarrhea.
- Limited absorption surface: Smaller than the small intestine, leading to incomplete absorption.
- Bowel evacuation: May promote defecation, reducing drug absorption.
- Microbial degradation: Drug can be degraded by rectal microflora.
Rectal Suppositories for Local Effect
- Used frequently to address local issues.
- Constipation: Laxatives like glycerin suppositories irritate the mucosa to induce bowel movement.
- Hemorrhoids: Hydrocortisone suppositories reduce pain, irritation, itching, and inflammation.
Anti-Hemorrhoidal Suppositories
- Often contain multiple components for comprehensive relief.
- Components: Local anesthetics, vasoconstrictors, astringents, analgesics, emollients, protective agents.
Rectal Suppositories for Systemic Actions
- Rectal mucosa allows absorption of soluble drugs for systemic effects.
- Vagina is less commonly used for systemic drug absorption.
Examples of Systemic Rectal Suppositories
- Nausea & vomiting: Ondansetron.
- Tranquilizers: Prochlorperazine and chlorpromazine.
- Opioid analgesia: Oxymorphone HCl.
- NSAID: Indomethacin.
- Analgesic & antipyretic: Paracetamol.
- Migraine: Ergotamine tartrate.
Factors Affecting Rectal Absorption
- Dosage variation: Can be higher or lower than oral dosage, influenced by various factors.
Physiologic Factors Affecting Rectal Absorption
- Colonic contents: An empty rectum enhances drug contact with the absorbing surface.
- Circulation route: Bypasses liver, leading to higher systemic effect for drugs metabolized by the liver.
- pH and buffering: Rectal fluids are neutral, minimally impacting drug stability.
Physicochemical Factors Affecting Rectal Absorption
- Lipid-water solubility: Lipophilic drugs are favored in fatty bases due to less escape into aqueous fluids.
- Drug concentration: Absorption plateaus beyond a certain concentration threshold.
- Particle size: Smaller particles increase surface area, promoting dissolution and absorption.
- Excipient: Must melt, soften, or dissolve at body temperature for drug release.
- Excipient-drug interactions: Interaction can hinder drug release and absorption.
Suppository Bases: Requirements
- Room temperature stability: Solid at room temperature.
- Body temperature melting: Melts, softens, or dissolves at body temperature to release the drug.
- Compatibility: No interactions with medication affecting stability or bioavailability.
- Long-acting formulations: Include materials like alginic acid for prolonged drug release.
Properties of Ideal Suppository Base
- Non-toxic: Safe for sensitive tissues.
- Inert: Does not interact with medication.
- Stable: Preserves integrity during storage.
- Manufacturability: Easily compressed or molded.
- Dissolution/disintegration: Dissolves or disintegrates in body fluids for drug release.
- Melting: Remains molten long enough to allow molding.
- Solidification: Rapid solidification for minimal sedimentation.
- Contraction: Contracts on cooling for easy removal from the mold.
- Wetting/emulsifying: Promotes drug release and absorption.
- Stability: Maintains shape, color, odor, and drug release pattern over time.
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Description
This quiz provides an overview of suppositories, including their advantages and disadvantages as solid dosage forms. Explore how these medications can be administered for both local and systemic effects, and understand the contexts in which they are beneficial. Test your knowledge on this important pharmaceutical topic.