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Flashcards in Midterm 1 Deck (26):
1

Pilocarpine

Selective muscarinic agonist.
Treats glaucoma by causing the contraction of ciliary muscles (M3 receptor) and increase in aqueous humor drainage.

2

Bethanechol

Selective muscarinic agonist (synthetic analogue).
Used to increase GI motility and bladder tone after surgery.

3

Atropine

Competitive muscarinic antagonist.
Used to dilate pupil, treat slow heart rate, and reduce secretion during surgery.

4

Ipratropium bromide

Competative muscarininc antagonist (synthetic analogue).
Treats asthma and COPD by dilating bronchi.

5

Muscarinic Agonists treat...

1. Glaucoma
2. Dry mouth
3. Stimulate tone in bladder after surgery
4. Increase gut motility

6

Side effects of muscarinic agonists...

Stimulates all muscarinic receptors, GI disturbances (nausea and vomiting), CNS effects, bradycardia, salivation and bronchoconstriction.

7

Nicotinic agonist uses and side effects

Used to treat nicotine addiction (patch, gum, aerosol).
Side effects (CNS): tremor, convulsions, coma

8

Curare

Nicotinic antagonist - non-depolarizing (competative) antagonist.
You can overcome blockade by increasing ACh with AChE inhibitor.
Used to produce skeletal muscle paralysis during surgery and in ICU.
Side effects: paralysis

9

Succinylcholine

Nicotinic antagonist - depolarizing (non-competative) antagonist.
You cannot overcome blockade by increasing ACh with AChE inhibitor.
Used to produce skeletal muscle paralysis during surgery and in ICU.

10

Neostigmine, physostigmine

Indirect acting cholinergic agent.
Inhibits metabolism of ACh in synapse (increases ACh duration).
Reversible cholinesterase inhibitor (weakly binds).
Uses: increases gut and bladder motility, treats glaucoma, treats myasthenia gravis.
Side effects: salivation, miosis, bronchoconstriction, bradycardia, nausea.

11

Insecticides (melathion) and nerve gases (sarin)

Irreversible cholinesterase inhibitor (covalent bond with AChE)
Effects at both muscarinic and nicotinic receptors.
Initial signs muscarinic (bronchoconstriction, salivation, GI symptoms, CNS symptoms). Followed byt CNS and PNS nicotinic signs (activation of skeletal muscle, paralysis).
Treatment: support respiration, decontamination, use muscarinic antagonist (atropine) and a compund that can break the covalent bond with the inhibitor (pralidoxime).

12

Differences between the 3 types of muscle.

Smooth: single nucleus, non striated, in walls of vessels and hollow organs, involuntary.
Cardiac: striated, single nucleus, branched, involuntary.
Skeletal: striated, multi nucleated, voluntary.

13

Types of receptors on presynaptic symp nerves, smooth muscles, heart, and other

Symp nerves: alpha 2
Smooth muscle: alpha 1 and beta 2
Heart: Beta 1
Other: alpha 2 and beta 2

14

Phenylephrine

Direct adrenergic alpha 1 agonist.
Treats: Nasal congestion (constricts bvs in nasal mucosa), dilates pupils (activates alpha 1 receptors), combines with local anesthetic (constricts bvs and prolongs nerve block).
Side effects: can increase BP

15

Clonidine

Direct adrenergic alpha 2 agonist.
Decreases release of NE via inhibition of AC and cAMP signalling.
Treats: hypertension
Side effects: sedation

16

Dobutamine

Direct adrenergic beta 1 agonist.
Treats: heart failure (increases the ability of the heart to contract)
Side effects: increased Ca can trigger arrhythmias

17

Salbutamol

Direct adrenergic beta 2 agonist.
Treats: asthma (relaxes smooth muscle via inhibition of MLCK phosphorylation and prevents bronchospasm), premature labour (relaxes pregnant uterus smooth muscle)
Side effects: increased HR (non specific activation of beta 1 in heart)

18

Adrenaline/Epinephrine

Direct adrenergic agonists (at multiple receptor subtypes).
Treat: anaphylaxis, and used in combo with anaesthetics
Side effects: Increased Ca can trigger arrythmias

19

Cocaine

Indirect adrenergic agonist.
Inhibits reuptake of NE.
Used for: anaesthetic (blocks Na channels in nerve), and topical anaesthesia in nasopharyngeal surgery
Side effects: CNS stimulant, increases HR/BP/FVC, arrhythmia

20

Amphetamine/ephedrine

Indirect adrenergic agonist.
Causes release of NA.
Treats: narcolepsy, ADHD, appetite surpressant
Side effects: CNS stimulant, increased HR/BP/FVC, arrhythmias

21

Phenoxybenzamine

Direct alpha adrenergic antagonist (block receptors in the SNS).
Non selective for a1 and a2.

22

Prazosin

Direct alpha adrenergic antagonist (block receptors in the SNS).
Selective for a1.
Treats: High BP
Side effects: hypotension, nasal congestion

23

Propanolol (non selective) and metroprolol (cardioselective b1)

Direct Beta antagonists.
Drugs that block B receptors in the SNS.
Treats: high BP, angina, arrhythmias, glaucoma (decrease aqueous humor secretion in eye).
Side effects: exercise tolerance, asthma

24

Beta-AR blockers and glaucoma

Act at Beta-AR receptors on the epithelium and decrease aqueous humor secretion leading to a decrease in pressure in the eye.
Gold standard.
Ex: propranolol

25

Cyclosporine

Given to people who have had an organ transplant to preserve the organ and stop their bodies from viewing it as foreign.
Increase susceptibility to infections (toxic reaction).
Kidney damage (side effect).
Rashes, hives, etc (allergic effect).
Inactivated by CP450

26

NTs and Receptors for...
1. PNS
2. SNS
3. Somatic
4. Sweat glands (SNS)
5. Adrenal medulla (SNS)

1. Pre: ACh N. Post: Ach M.
2. Pre: Ach N. Post: NE alpha and beta.
3. One neuron: ACh N.
4. Pre: Ach N. Post: Ach M.
5. Pre: ACh N. Releases: NE and Adr.