Cardiovascular Pharmacology Summary Part 5 Flashcards
Which drugs are reversible parasympathomimetics?
Neostygmine
Pyridostigmine
Pilocarpine
What agent is an irreversible parasympathomimetic?
Malathion
What is the mechanism of action of the reversible parasympathomimetics (cellular)?
Indirectly increases acetylcholine levels by inhibiting acetylcholine esterase. This is a reversible inhibition. The increases in Ach stimulate muscarinic receptors in the PSNS and somatic motor neuron end plate.
What is the mechanism of action of the irreversible parasympathomimetics (cellular)?
Indirectly increases acetylcholine levels by inhibiting acetylcholine esterase irreversibly. The increases in Ach stimulate muscarinic receptors. All post ganglionic receptors on GIT and bronchial muscle are stimulated.
What is the mechanism of action of the irreversible parasympathomimetics (physiological)?
Generally - miosis, increases peristalsis, increased bladder voiding, slows heart rate, bronchoconstriction & mucous production, salivary production.
What is the mechanism of action of the reversible parasympathomimetics (physiological)?
Generally - miosis, increases peristalsis, increased bladder voiding, slows heart rate, bronchoconstriction. Neosygmine / pyridostigmine - reversible Ach esterase inhibitor.
What are the therapeutic uses of the reversible parasympathomimetics?
Treatment of myasthenia gravis and surgical ileus.
Rivastigmine (central Ach esterase inhibitor) used for Alzheimer’s.
What is malathion?
This is a highly toxic pesticide with marked effects on mammalian physiological processes.
What is the antidote for malathion poisoning?
Atropine
What are the adverse effects of the parasympathomimetic agents?
- Asthma
- Diarrhea
- Salivation
- Bradycardia
* In malathion poisoning patients down in bronchiole secretions.
What is the mechanism of action of pilocarpine (cellular)?
Generally, miosis
- opens trabecular network by stimulating muscarinic receptors in the canal of Schlemm.
What is the mechanism of action of pilocarpine (physiological)?
Stimulates muscarinic receptors as a muscarinic agonist.
- The opening of the trabecular network of the eye allows outflow of aqueous humor.
What are the therapeutic uses of pilocarpine?
Glaucoma!
- Aqueous humor outflow lowers intraocular pressure and is used in conjunction with other preparations.
What are the adverse effects / contraindications of pilocarpine?
- Asthma
- Diarrhea
- Salivation
- Bradycardia
Which drugs are parasympatholytics?
Atropine
Hyoscine
Ipratropium Bromide
How is Ipratropium Bromide administered?
By MDI or nebulization
What is the mechanism of action of atropine and hyoscine (cellular)?
Generally, decrease salivation, mydriasis, decreases peristalsis, prevent bladder voiding, increase heart rate, decrease salivary gland secretion, increase bladder sphincter tone
What is the mechanism of action of atropine and hyoscine (physiological)?
Blocks post ganglionic muscarinic receptors. Also causes cycloplegia (paralysis of ciliary muscles) leading to a failure to accommodate for near vision.
What is atropine used for?
Used to stop vagal induced effects and decrease salivation as a premed in surgery
What is hyoscine used for?
Irritable bowel syndrome especially with cramping and diarrhea
What are the adverse effects / contraindications of atropine and hyoscine?
- Dry mouth
- Tachycardia
- Constipation
- Urine retention
- Blurred vision
- Mydriasis
- Glaucoma
What is the mechanism of action of Ipratropium Bromide (cellular)?
Blocks post ganglionic muscarinic receptors in the bronchioles.
What is the mechanism of action of Ipratropium Bromide (physiological)?
Causes bronchodilation, allowing for improved air outflow in asthma and COPD.
What are the therapeutic uses of Ipratropium Bromide?
Used for asthma as a MDI, as well as in obstructive airway diseases like COPD. Also decreases mucous production. Not as effective in asthma and usually reserved for more severe asthmatic cases. Used mainly in adult onset asthma and COPD which has a higher cholinergic component.
What are the adverse effects / contraindications of Ipratropium Bromide?
- Dry mouth
- Tachycardia
- Constipation
- Urine retention
- Blurred vision
- Mydriasis
- Glaucoma