[MEDORG-SEMIS-04-PT2] CHOLINERGIC

THIS FLASHCARDS IS ABOUT [MEDORG] CHOLINERGIC - ANTI-MUSCARINIC AGENTS.

Supplemental Info Only

PHARMACOPHORE OF MUSCARINIC ANTAGONISTS:

Typical structure contains:

1. Aromatic ring

2. Ester linkage

3. Tertiary amine

4. Bulky substituents

Supplemental Info Only

General pharmacophore:

Ar — C — O — CH2 — CH2 — N(R)2

(Bulky groups prevent receptor activation but allow binding)

Bulky groups

SAR Principles of Anti-Muscarinic Agents:

Large substituents increase antagonist activity.

Aromatic rings

SAR Principles of Anti-Muscarinic Agents:

Increase lipophilicity and receptor binding.

Tertiary Amines

SAR Principles of Anti-Muscarinic Agents:

Cross blood-brain-barrier.

Quaternary Ammonium Compounds

SAR Principles of Anti-Muscarinic Agents:

Limited CNS penetration.

Ipratropium

This drug has quaternary nitrogen, limiting systemic effects.

• Atropine

• Scopolamine

• Benztropine

• Ipratropium

• Oxybutynin

What are the (5) Examples of Anti-Muscarinic Drugs?

Hint: AS-BIO

Atropine

This drug is a prototype muscarinic antagonist.

Structure:

• Tropane ring

• Aromatic ester

• Mydriasis

• Tachycardia

• Decreased secretions

What are the (3) Effects of Atropine?

Hint: MTD

Mydriasis

This is the dilation of the pupil, which can be normal or abnormal depending on the cause.

Tachycardia

This is an abnormal heart rhythm with a fast heart rate of more than 100 beats per minute at rest.

Scopolamine

This drug is similar to atropine but more CNS penetration.

Motion sickness

Scopolamine is used for?

Benztropine

This anti-muscarinic drug is an anticholinergic used in Parkinson Disease.

Parkinson Disease

Benztropine is used for what disease?

Two aromatic rings

Benztropine contains ____________, increasing lipophilicity.

Ipratropium

This drug is a quaternary ammonium compound.

True

True or False: Ipratropium cannot cross the blood-brain-barrier.

Bronchodilator

In COPD, Ipratropium is used as?

Oxybutynin

This antimuscarinic drug is used for overactive bladder.

Structure designed to: Reduced smooth muscle contractions.

Overactive bladder

Oxybutynin is used for?