Question

5. Some of the antimuscarinics can cross the blood–brain barrier. What are the properties of a drug that would make them more likely to cross the blood–brain barrier?

6. What symptoms could be reported as adverse side effects in a drug that was able to cross the blood–brain barrier?

7. Some of the antimuscarinic agents are metabolised by the cytochrome P450 enzymes. Drawing on your knowledge of these important metabolising enzymes, explain the effect of the cytochrome P450 enzymes

8. List some of the drugs or foods that could interfere with the metabolism of the antimuscarinic agents.

9. Bearing in mind Lorraine’s identification of the most bothersome urinary incontinence symptom, what would be your choice of first-line management for her?

10. With reference to their pharmacological properties, describe how antimuscarinics can lead to the side effects of dry mouth and constipation.

11. Contraindications to the use of antimuscarinic drugs are all of the following except:

a) Glaucoma

b) Myasthenia

c) Bronchial asthma

d) Paralytic ileus and atony of the urinary bladder


12. Adverse peripheral effects, such as loss of accommodation, dry mouth, tachycardia, urinary retention, constipation are related to:

a) Alpha adrenoreceptor blockade

b) Muscarinic cholinoreceptor blockade

c) Supersesitivity of the dopamine receptor d) Dopamine receptor blockade

13. Please create a drug card for:

Oxybutynin

Duloxetine

Imipramine

Answer 1

(5)Overactive bladder (OAB) is a shared disorder, chiefly in the ageing. Anticholinergic agents are the backbone of pharmacological action of OAB; though, many anticholinergics can cross the blood-brain barrier (BBB) and might reason central nervous system (CNS) effects, counting cognitive shortfalls, which can be particularly harmful in adult patients. Many anticholinergics have the possible to reason opposing CNS effects due to muscarinic receptor requisite in the brain. Of memo, penetrability of the BBB upsurges with phase and can also be pretentious by strain, pressure, and some illnesses and medicines. Passive journey of a molecule crossways the BBB into the brain is reliant on upon its physicochemical properties.

(6) Older peoples are at healthier hazard for the anticholinergic side effects, and dry mouth. An advanced absorption in the brain since of variations in absorption and removal, there are variations in the blood-brain barrier, your brain gets additional leaking and such that extra leaves the capillary receiving into your brain.

(7) Cytochrome P450 enzymes are vital for the breakdown of many medicines. Though this has extra than 50 enzymes, , with the two most significant enzymes existence CYP3A4 and CYP2D6.

(8)A high fat meal, grapefruit, high calorie meal. Drugs like Mirabegron and Trospium.

(9) The organization of UI should comprise an assessment of possible revocable donors and hearings of nonpharmacological interferences, which be contingent on the type of UI recognized. Clinical educations provision proper nourishment, the evasion of constipation, weight loss, and physical movement as helpful in refining symptoms.

(10) Most mutual adverse proceedings related with oral antimuscarinics are dry mouth and constipation; the occurrence of central nervous system (CNS) side effects is squat and alike to that with palliative. Native adverse skin responses are the most usually reported side result with the oxybutynin transdermal distribution scheme (OXY-TDS).

(11)Glaucoma - Even reasonable amounts of drugs with antimuscarinic effects assumed systemically can persuade acute glaucoma in patients with low anterior eye cavities.

(12) Alpha adrenoreceptor blockade - when managed systemically, it provokes the “break and digest” effects shaped by the parasympathetic nervous system.