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Questions and Answers
What are suppositories intended for?
What are suppositories intended for?
What is the main advantage of using suppositories?
What is the main advantage of using suppositories?
They can be used when oral medication is not possible.
Suppositories are suitable for patients suffering from diarrhea.
Suppositories are suitable for patients suffering from diarrhea.
False
What is the weight of adult suppositories?
What is the weight of adult suppositories?
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Which of the following is not a type of rectal suppository?
Which of the following is not a type of rectal suppository?
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What are urethral suppositories for males typically weighted?
What are urethral suppositories for males typically weighted?
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The rectum is part of the _____ and forms the last 15-20 cm of the GI tract.
The rectum is part of the _____ and forms the last 15-20 cm of the GI tract.
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Match the type of suppository with its description:
Match the type of suppository with its description:
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What are suppositories?
What are suppositories?
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Which of the following is NOT a use of suppositories?
Which of the following is NOT a use of suppositories?
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Suppositories can be beneficial for patients who cannot swallow oral medication.
Suppositories can be beneficial for patients who cannot swallow oral medication.
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What is one disadvantage of rectal suppositories?
What is one disadvantage of rectal suppositories?
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What is the typical weight of suppositories for adults?
What is the typical weight of suppositories for adults?
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What is the pH of mucus in the rectum?
What is the pH of mucus in the rectum?
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Which blood vessel returns blood from the rectum to the liver?
Which blood vessel returns blood from the rectum to the liver?
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The main blood supply to the rectum comes from the __________.
The main blood supply to the rectum comes from the __________.
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What are the shapes typically associated with vaginal suppositories?
What are the shapes typically associated with vaginal suppositories?
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Drugs absorbed via rectal administration undergo first-pass metabolism.
Drugs absorbed via rectal administration undergo first-pass metabolism.
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Study Notes
Suppositories
- Single-dose preparations inserted into body orifices like the rectum, vagina, urethra, ear, or nose
- Melt or dissolve to release the drug for local or systemic action
- Consist of the drug incorporated into an inert vehicle (base)
- Fatty bases melt at body temperature, hydrophilic bases dissolve in mucous secretions
Applications of Suppositories
- Pain and itching relief, especially due to hemorrhoids
- Locally active drugs: astringents, antiseptics, local anesthetics, vasoconstrictors, anti-inflammatory compounds, soothing & protective agents, and some laxatives
Advantages of Suppositories
- Ideal for babies, elderly, post-operative patients who cannot swallow oral medication
- Suitable for patients with severe nausea or vomiting
- For drugs inactivated by stomach pH or enzymatic activity
- For drugs irritating to the stomach
- For drugs destroyed by portal circulation
Disadvantages of Rectal Suppositories
- Patient acceptance can be a problem
- Not suitable for patients with diarrhea
- Irritant drugs may require excessive dosage
- Proctitis (rectal inflammation) is a potential side effect
- Large-scale production may be challenging, and shelf-life can be a concern
- Slow and incomplete absorption due to:
- Interruption by defecation, especially with irritant drugs
- Small surface area of the rectum compared to the small intestine
- Lower fluid content in the rectum compared to the small intestine
- Microbial degradation can occur in the rectum
Types of Suppositories by Route of Administration
- Rectal: Conical or torpedo-shaped, 2-3 cm long, 2 grams for adults, 1 gram for children
- Urethral: 4 grams for males, 2 grams for females
- Vaginal (pessaries): Globular, oviform, or cone-shaped, 3-5 grams
- Nasal bougies: Thin and pencil-shaped with pointed ends, 1-2 grams, 9-10 mm long
- Ear cones: Also pencil-shaped
Anatomy and Physiology of the Rectum
- Last 15-20 cm of the gastrointestinal tract
- Hollow organ with a flat wall surface, lacking villi
- Estimated mucus volume of 3 ml, pH of 7.5, surface area of 300 cm2
- Lack of villi indicates limited primary absorptive function, drug passage occurs via passive diffusion
Rectal Blood Circulation
- Main blood supply: Superior rectal artery
- Blood return via three veins:
- Superior (upper) hemorrhoidal vein
- Middle hemorrhoidal vein
- Inferior (lower) hemorrhoidal vein
- Superior hemorrhoidal vein flows to the inferior mesenteric vein, then to the hepatic portal vein, and finally to the liver
- Middle and inferior hemorrhoidal veins bypass the liver, leading to direct systemic circulation
- This bypass avoids first-pass metabolism by the liver and allows the drug to bypass the stomach and digestive enzymes
Course Contents
- Suppositories - 3 lectures
- Powders and Granules - 1 lecture
- Tablets - 3 lectures
- Capsules - 2 lectures
- Reaction Kinetics - 3 lectures
Weighting of Assessments
- Final Examination - 50%
- Oral Examination - 10%
- Practical Examination - 25%
- Quizzes and Assignments - 15%
Quizzes
- First week 4th
- Second week 8th
Course Learning Outcomes (CLOs)
- Illustrate different types of suppositories, capsules, powdered dosage forms, granules, and tablets, as well as excipients used in their preparation.
- Show the importance of physicochemical properties of drugs during the design of different dosage forms.
Suppositories
- Definition: Single-dose preparations intended for insertion into body orifices, such as the rectum, vagina, urethra, and sometimes ear or nose.
- Purpose: To melt or dissolve, releasing the drug to exert local or systemic action.
- Composition: Drug incorporated into an inert vehicle (base).
- Bases: Fatty bases melting at body temperature or hydrophilic bases slowly dissolving in mucous secretions.
Application of Suppositories
- Pain and Itching Relief: Used for conditions like hemorrhoids, with drugs like antiasthmatics, antirheumatic, and analgesics.
- Locally Active Drugs: Astringents, antiseptics, local anesthetics, vasoconstrictors, anti-inflammatories, soothing and protective agents, and some laxatives.
Advantages of Suppositories
- Alternative to Oral Administration: Ideal for babies, elderly individuals, post-operative patients, those experiencing nausea or vomiting, or those with conditions where oral medications are ineffective.
- Bypass Stomach and Intestine: Administer drugs inactivated by stomach pH or enzymatic activity, or drugs that irritate the stomach.
- Avoid First-Pass Metabolism: Drugs that are destroyed by portal circulation can be administered rectally.
Disadvantages of Rectal Suppositories
- Patient Acceptability: Some patients may find it uncomfortable.
- Diarrhea: Not suitable for patients with diarrhea.
- Irritation: Amount of drug needed may be irritating or too large for a suppository.
- Proctitis: Risk of developing inflammation of the rectum
- Production Challenges: Difficult to achieve a suitable shelf-life.
-
Incomplete Absorption:
- Defecation can interrupt absorption.
- The surface area of the rectum is smaller than the small intestine.
- The fluid content of the rectum is less than the small intestine, affecting drug dissolution.
- Microbial degradation can occur in the rectum.
Types of Suppositories by Route of Administration
- Rectal: Conical or torpedo shape, 2-3 centimeters long, 2 grams for adults and 1 gram for children.
- Urethral: 4 grams for males and 2 grams for females.
- Vaginal (Pessaries): Globular, oviform, or cone-shaped, 3-5 grams.
- Nasal Bougies: Thin pencil shape with pointed ends, 1-2 grams, 9-10 mm long.
- Ear Cones: Pencil shape.
Anatomy and Physiology of the Rectum
- Location: Last 15-20 cm of the gastrointestinal (GI) tract.
- Structure: Hollow organ with a relatively flat wall surface, lacking villi.
- Mucus: 3 ml of mucus with pH of 7.5, covering a surface area of 300 cm2.
- Absorption: No villi indicate no primary absorptive function; drug passage occurs by passive diffusion.
Rectal Blood Circulation
-
Main Blood Supply: Superior rectal artery.
-
Blood Return: Three main veins:
- Superior (upper) hemorrhoidal vein
- Middle hemorrhoidal vein
- Inferior (lower) hemorrhoidal vein
-
Venous Drainage Pathways:
- Superior Hemorrhoidal Vein: Inferior mesenteric vein -> Hepatic portal vein -> Liver
- Middle and Inferior Hemorrhoidal Vein: Directly into systemic circulation, bypassing the liver.
- Implications: Drugs administered rectally avoid the first-pass metabolism of the liver.
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Description
Explore the world of suppositories, including their composition, applications, advantages, and disadvantages. Understand how these single-dose preparations provide medication through various body orifices and their significance in patient care, especially for those unable to take oral medications.
