[PCOL-SEMIS-01-PT8] AUTACOIDS: CLINICAL USES

THIS FLASHCARDS IS ABOUT [PCOL] AUTACOIDS.

First Generation

What generation of H₁-antagonists is the most effective for the prevention and treatment of allergic reactions?

• Parkinsonism

• EPS

First Generation H₁-antagonists is used for the management of?

Parkinson’s Disease (Parkinsonism)

A neuro degenerative disease due to the imbalance in neurotransmitter.

Supplemental Info Only

In Parkinsonism, there is an increase in the number of Acetylcholine inducing a cholinergic effect and a decrease in Dopamine, which is an indication of Parkinson’s Disease.

Supplemental Info Only

First Generation Antihistamine is used as its effect is anticholinergic.

1. Extrapyramidal Symptoms

2. Antipsychotics

EPS stands for (1)_________; caused by (2)________.

• Akathisia

• Pseudo Parkinsonism

• Acute Dystonia (Torticollis)

What are the (3) Types/Manifestation of EPS?

Hint: APA

Akathisia

This manifestation of EPS is the restlessness or uncontrollable movement.

1. Acute Dystonia

2. Torticollis

(1) This manifestation of EPS is the is also known as (2)_____ or the twisting of neck (stiff neck).

Anticholinergic

(Anticholinergics are generally not effective for akathisia)

EPS: In acute dystonia and pseudo parkinsonism, this classification of drugs is used.

1. Ethanolamines

2. Unisom®

First Generation H₁-antagonists are useful as sleeping aids specifically the (1)_____, in the brand name (2)_____.

1. Gel or tablet form

2. Diphenhydramine

3. Doxylamine

Unison® can be in a (1)________ form because it contains (2)_____ or (3)_____.

1. Motion sickness

2. Meclizine

3. Cyclizine

First Generation H₁-antaganists is used as a management of (1)__________. Two examples are (2-3)__________.

1. Cold preparations (alkylamines)

2. Brompheniramine

3. Chlorpheniramine

First Generation H₁-antaganists is used as a component of (1)__________. Two examples are (2-3)__________.

1. Anesthetic adjuncts

2. Promethazine

First Generation H₁-antaganists is used as (1)_________, an examples is (2)_____.

1. 5-HT syndrome

2. Cyproheptadine

First Generation H₁-antaganists is used as a management of (1)____ syndrome, an example is (2)_____.

Supplemental Info Only

Adverse Effects of H₁-Antagonists:

• Sedation (mostly first generation)

• Anticholinergic effects (opposite of DUMBELS)

Cardiotoxicity

Adverse Effect of H₁-Antagonists:

Fexofenadine when combined with enzyme inhibitors (CYP3A4), Terfenadine, and Astemizole, leads to arrythmias.

1. Fexofenadine

2. CYP3A4

3. Terfenadine

4. Astemizole

5. Arrythmias

Cardiotoxicity: (1)________ when combined with enzyme inhibitors like (2-4)__________, leads to (5)_____.

• Terfenadine

• Astemizole

(They are withdrawn from the market because they inhibit the enzyme for metabolism of Fexofenadine)

These two are antimicrobials.

Supplemental Info Only

If the metabolism of Fexofenadine is prevented, it will accumulate in the blood (high concentration) and causes QT prolongation of ECG.

• Cimetidine

• Ranitidine

• Nizatidine

• Famotidine

What are the (4) Drugs under H₂-Antagonists?

Hint: CRNF

Gastric Acid

H₂-antagonists inhibits the secretion of?

Cimetidine

H₂-antagonists: This drug is less potent.

Zantac®

H₂-antagonists: Ranitidine is marketed under what brand name?

Nizatidine

H₂-antagonists: This is the only drug taken orally.

Famotidine

H₂-antagonists: This drug is the most potent.

1. Gastroesphageal reflux disease (GERD)

2. Proton-pump inhibitors (PPIs)

CLINICAL APPLICATIONS OF H₂-ANTAGONISTS:

Management of (1)___________; the first line is (2)_____ because it is the most effective one.

1. Acid peptic diseases

2. Proton-pump inhibitors (PPIs)

CLINICAL APPLICATIONS OF H₂-ANTAGONISTS:

Management of (1)__________; the first line is (2)_____.

1. GI ulcer bleeding

2. Intravenous

CLINICAL APPLICATIONS OF H₂-ANTAGONISTS:

First line in the management of acute (1)__________ and is administered (2)_____.

Supplemental Info Only

H₂-antagonists can be an adjunct in the management of allergic reactions.

True

True or False: H2 blockers can be taken with H1 blockers.

1. Cimetidine

2. Galactorrhea

ADVERSE EFFECTS OF H₂-ANTAGONISTS:

• Enzyme inhibition; an example is (1)_____.

• Anti-androgenic effects

• Increase (2)______.

1. Anti-androgenic effects

2. Dihydrotestosterone

This (1) effect inhibits the binding of (2)__________ to androgen receptors.

Codeine

What is the prodrug of morphine?

Supplemental Info Only

If cimetidine is administered together with codeine, there is a sub-therapeutic. Cimetidine inhibits the enzyme that metabolize codeine to its active form (morphine; high analgesic effect).

Cimetidine

What is the drug responsible for the anti-androgenic effects?

Gynecomastia

Cimetidine inhibits binding of dihydrotestosterone to androgen receptors resulting to the enlargements of breasts among the males.

Galactorrhea

Increase prolactin levels.