DRUGS Flashcards

1
Q

TTX

A

Na+ channel inactivation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
2
Q

TEA

A

K+ channel inactivation, but non selective so it can target Ca2+ channels and also target the nAChRs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
3
Q

Cocaine

A

Agonist of NA+ channels in use dependent competitive manner - 3% actually binds to Na+ channels O’Leary 2010 - joyous feelings arise from the indirect agonist of dopamine reuptake receptors (DAT)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
4
Q

Derivatives of cocaine used because

A

Coke takes ages to unbind from Na+ receptors - and hence the effects cannot be appropriately mediated - 8x slower - Crumb and Clarkson 1990

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
5
Q

3 major discoveries of the synapse

A

1936 Loewi and Dale NP - demonstrated that transmission was chemical
Loewi - placed two frog hearts in a bath and slowed the first - the second slowed two and determined the substance was Vagustoff
Dale then determined this was ACh with experiments on leech muscle

Vesicles - then from the coloured with histochemical staining then electron microscopy - Koelle et Al - 1949

Fatt and Katz - 1954 - determined the vesicular and quantal nature of ACh release - mEPPs - determined too big to be of just one ACh molecule and that they were uniform in size

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
6
Q

Turbocuraine

A

NMJ - Non depolarising competitive antagonist of nAChRs - long duration paralytic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
7
Q

Suxamethonium

A

Depolarising direct cholinergic agonist - intermediate fasiculation

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
8
Q

Sarin nerve gas

A

Inhibits by competitive binding AChE - seizures and resp arrest

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
9
Q

Organophosphates

A

AChE inhibitors also excess muscarinic and nicotinic action

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
10
Q

Botulinum toxin

A

Cleaves SNAP 25 - no partial fusion so no vesicular release

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
11
Q

Myaesthenia Gravis

A

IgG autoantibodies - bind to and increase the rate at which the receptor itself is degraded - treated with AChEs

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
12
Q

Atropine

A

Anticholinergic muscarinic competitive antagonist - acts on M2 (inhibits an inhibitory) - at vagus nerve junction

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
13
Q

Pirenzepine

A

Muscarinic M2 receptor antagonist - inhibits gastric acid secretion

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
14
Q

Gallamine

A

M2 competitive antagonist - muscle relaxation in general anaesthetic

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
15
Q

Darifenacin

A

M3 agonist located in smooth muscle (bladder)

How well did you know this?
1
Not at all
2
3
4
5
Perfectly
16
Q

Hess experiment

A

1920s - invented interrupted DC and paced it through a cats brain - could induce higher HR and a generalised stress state - termed the region the arcuate nucleus of the hypothalamus

17
Q

Alpha 1 both

A

Gq
Agonist - phenylephrine - activation of α1-adrenoceptors in the arterioles of the nasal mucosa. This causes vasoconstriction, which leads to decreased edema and increased drainage of the sinus cavities.

Antagonist - prazosin - relaxed muscle, including blood vessels and therefore lowers blood pressure

18
Q

Alpha 2 both

A

Gi
Agonists - methyldopa antihypertensive - all normally oppose the effects of the sympathetic nervous system to produce sedation, analgesia, and euphoric effects and partially block acute withdrawal symptoms in chronic opioid users

Antagonist - mirtazapine - dual mode of action. It is a noradrenergic and specific serotonergic antidepressant (NaSSA) that acts by antagonising the adrenergic alpha2-autoreceptors and alpha2-heteroreceptors and increase sympathetic action

19
Q

Beta 1 both

A

Gs
Agonist - dobutamine - inotropic effect increases contractility, leading to decreased end-systolic volume and, therefore, increased stroke volume

Antagonist - metoprolol - cardiac output by negative inotropic and chronotropic effects and decreases sympathetic activity

20
Q

Beta 2 both

A

Gs
Agonist - albuterol - relaxes the bronchial smooth muscle. It also inhibits the release of immediate hypersensitivity mediators from cells, especially mast cells to treat/ prevent bronchospasm

No selective beta 2 antagonists

21
Q

M3

A

Agonist - Pilocarpine - By directly stimulating these receptors, pilocarpine causes smooth muscles, such as the iris sphincter muscle and ciliary muscle, to contract

Antagonist - tiotropium - bronchodilation by relaxing and opening the air passages to the lungs to make breathing easier

22
Q

M1

A

Agonist - sabcomeline - though in spite of important cognitive enhancing effects, most trials have been discontinued due to considerable side-effects

Antagonist - scopolamine - central nervous system (CNS) to create a calming effect on the muscles in the stomach and bowels (gut) post anaesthesia anti-nausea