Cholinergic & Anticholinergics

Question 1

Indirect- Acting Cholinergic Agonists used to treat Myasthenia Gravis:

Answer 1

Neostigmine: Has a strong influence at the neuromuscular junction.

Pyridostigmine: Has a longer duration of action that neostigmine.

Edrophonium: Diagnostic agent for Myasthenia Gravis.

Question 2

Indirect- Acting Cholinergic Agonists used to SLOW Alzheimer’s Disease:

Answer 2

Glanatamine and Rivanstigmine (Oral Solution)

Donepezil(Once-a-day dosing)

Question 3

Indirect-Acting Cholinergic Agonists ACTIONS:

Answer 3

Block AChE at the synaptic cleft, allowing build up of ACh released from the nerve endings and leads to increased and prolonged stimulation of ACh.

Question 4

Indirect-Acting Cholinergic Agonists INDICATIONS:

Answer 4

Myasthenia Gravis
Alzheimer’s Disease
Treatment after exposure to nerve gas (Chemical Warfare)

Question 5

Indirect-Acting Cholinergic Agonists ADVERSE EFFECTS:

Answer 5

Adverse Effects:
Bradycardia, hypotension.
Increased GI secretions and activity.
Increased bladder tone.
Bronchoconstriction.
Relaxation of GI and genitourinary sphincters.
Pupil Constriction.

Question 6

Indirect-Acting Cholinergic Agonists DRUG-DRUG INTERACTIONS:

Answer 6

NASID’s and Cholinergic drugs.

Question 7

Indirect-Acting Cholinergic Agonists CONTRAINDICATIONS:

Answer 7

ALLERY
Bradycardia
Intestinal or urinary tract obstruction.

Question 8

Indirect-Acting Cholinergic Agonists CAUTIONS:

Answer 8

Any condition that could be exacerbated by Cholinergic stimulation:
Asthma
Coronary Disease
Peptic Ulcer
Arrhythmias
Epilepsy or Parkinsonism
Hepatic or Renal dysfunction.
Pregnancy or lactation.

Question 9

Anticholinergic Agents:

Answer 9

Atropine, Dicyclomine, Glycopyrrolate, Ipratropium, Meclizine, Oxybutynin, Scopolamine, Titropium, Tolterodine.

Question 10

Anticholinergic Agents ACTION:

Answer 10

Blocks the acetylcholine receptors at the muscarinic Cholinergic receptor site.

Question 11

Anticholinergic Agents INDICATIONS:

Answer 11

Decreased Secretions.
Decreased Bronchospasm.
Restore cardiac rate and blood pressure.
Pylorospasm and hyperactive bowel.
Relax uterine hypertonicity.
ATROPINE - Administered as an antidote to Cholinergic crisis (Overdose).

Question 12

Anticholinergic Agents ADVERSE EFFECTS:

Answer 12

Blurred vision / Mydriasis.
Cycloplegia
Photophobia
Palpatations/ tachycardia.
Dry mouth/ altered taste perception.
Constipation
Decreased sweating; predisposition to heat exhaustion.

Question 13

Anticholinergic Agents DRUG-DRUG INTERACTIONS :

Answer 13

Any other drug with anticholinergic activity: Antihistamines, antiparkinsonism drugs, MAOI’s, and TCA’s.
Phenothiazines
Herbal Therapies.

Question 14

Anticholinergic Agents CONTRAINDICATIONS:

Answer 14

ALLERGY / HYPERSENSITIVITY.
Any condition that can be exacerbated by blocking the PNS: Glaucoma, stenosisng peptic ulcer disease, prostatic hypertrophy, bladder obstruction.

Question 15

Anticholinergic Agents CAUTIONS:

Answer 15

Cardiac Arrhythmias, tachycardia, myocardial ischemia.
Impaired liver of kidney function.
Hypertension
Pregnancy or lactation
Spasticity or brain damage.

Question 16

Direct- Acting Agonists (Nicotinic):

Answer 16

Bupropion
Nicotine
Varenicline

Question 17

Direct-Acting Cholinergic Agonists (Nicotinic) ACTIONS:

Answer 17

Bupropion: May act by weakly inhibiting neuronal reuptake of Norepinepherine and dopamine.

Nicotine: Replacement Therapy.

Varenicline: Acts as nicotine receptor partial agonist.

Question 18

Direct- Acting Cholinergic Agonists (Nicotinic) INDICATIONS:

Answer 18

Smoking Cessation.

Question 19

Direct-Acting Cholinergic Agonists (Nicotinic) ADVERSE EFFECTS:

Answer 19

Tachycardia, hypertension.
Nausea, dry mouth.
Skin rash.
Seizures, neuropsychiatric adverse effects, dizziness, strange dreams.

Question 20

Direct-Acting Cholinergic Agonists (Nicotinic) DRUG-DRUG INTERACTIONS:

Answer 20

NUMEROUS drug-drug interactions.

Question 21

Direct-Acting Cholinergic Agonists (Nicotinic) CONTRAINDICATIONS:

Answer 21

Hypersensitivity/ Allergy.
Seizure Disorder (Bupropion).

Question 22

Direct-Acting Cholinergic Agonists (Nicotinic) CAUTIONS:

Answer 22

Pregnancy and lactation.

Question 23

Direct- Acting Cholinergic Agonists (Muscarinic):

Answer 23

Bethanechol, Carbachol, Cevimeline, Pilocarpine.

Question 24

Direct- Acting Cholinergic Agonists (Muscarinic) ACTIONS:

Answer 24

Act at Cholinergic receptors in the nervous system to mimic the effects of ACh and the parasympathetic stimulation.

Question 25

Direct- Acting Cholinergic Agonists (Muscarinic) INDICATIONS:

Answer 25

Bethanechol: Urinary retention. Carbachol: Induce miosis. Cevimeline and Pilocarpine: Treat dry mouth.

Question 26

Direct- Acting Cholinergic Agonists (Muscarinic) ADVERSE EFFECTS:

Answer 26

Nausea, vomiting, cramps, diarrhea, increased salivation and involuntary defecation. Bradycardia, heart block, hypotension. Urinary urgency. Flushing or increased sweating.

Question 27

Direct- Acting Cholinergic Agonists (Muscarinic) DRUG-DRUG INTERACTIONS:

Answer 27

Acetylcholinesterase inhibitors.

Question 28

Direct- Acting Cholinergic Agonists (Muscarinic) CONTRAINDICATIONS:

Answer 28

Hypersensitivity/ Allergy. Any condition that can be exacerbated by parasympathetic effects: Bradycardia, hypotension. Peptic Ulcer disease, intestinal obstruction or recent GI sx. Asthma Bladder Obstruction. Epilepsy and Parkinsonism.

Question 29

Direct- Acting Cholinergic Agonists (Muscarinic) CAUTIONS:

Answer 29

Pregnancy and Lactation.