CR2 KCP 2 - Response to xenobiotics Flashcards

1
Q

Alpha 1 receptors location & function

A
  • Vascular smooth muscles, smooth muscles around neck of bladder & prostate, GI sphincters, radial iris muscle
  • Contraction
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2
Q

Alpha 2 receptors location & function

A
  • Presynaptic neuron, pancreas
  • Inhibition of neurotransmitter release, decrease insulin
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3
Q

Beta 1 receptors location & function

A
  • Heart & kidney
  • Myocardial stimulation, renin release
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4
Q

Beta 2 receptors location & function

A
  • Respiratory, uterine & vascular smooth muscle, liver, pancreas, muscle spindles
  • Smooth muscle relaxation, glycogenolysis, increase glucagon, tremors
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5
Q

Beta 3 receptors location & function

A
  • Adipose tissue
  • Lipolysis
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6
Q

D 1 receptors location & function

A
  • Renal vascular smooth muscles
  • Dilation
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7
Q

D 2 receptors location & function

A

Nerve endings in the CNS & GIT
- Modulation of transmitter release, CNS stimulation

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8
Q

Sympathomimetic classes

A
  1. Direct acting (selective & non-selective)
  2. Mixed acting
  3. Indirect acting (releasing agent, uptake inhibitor & MAO/COMT inhibitor)
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9
Q

Non-selective alpha blocker

A

Reversible: Phentolamine
Irreversible: Phenoxybenzamine

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10
Q

Selective alpha blockers

A

Alpha 1: Prazosin
Alpha 2: Yohimbin

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11
Q

Non-selective beta blocker with no ISA

A

Propranolol

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12
Q

Selective beta 1 blockers

A

with ISA: Pindolol (non-selective)
without ISA: Metoprolol

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13
Q

Alpha + Beta blocker

A

Labetolol

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14
Q

Direct acting cholinergic agonists

A

M&N: Acetylcholine
M: Pilocarpine, Methacholine
N: Nicotine, Succinyl choline (Suxamethonium chloride)

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15
Q

Reversible indirect acting Cholinesterase inhibitors

A

Short-acting: edrophonium
Medium-duration: neostigmine (proserine), physostigmine (eserine)

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16
Q

irreversible indirect acting Cholinesterase inhibitors

A

Organophosphates:
- Soman & Sarin (nerve gas)
- Malathion (insecticide)

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17
Q

Muscarinic blockers

A
  • Atropine
  • Scopolamine
  • Ipratropium
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18
Q

Nicotinic blockers

A
  • D-tubocurarine
  • Succinylcholine
  • Mecamylamine
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19
Q

Narrow therapeutic index drugs

A
  • Barbiturates
  • Theophylline
  • Cardiac glycosides
  • Warfarin
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20
Q

Wide therapeutic index drugs

A
  • Benzodiazepines (e.g. Diazepam)
  • Penicillin
  • Cephalosporines (e.g. Cefadoxil)
  • Acetaminophen (e.g. Paracetamol)
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21
Q

Adverse drug reaction (ADR) types

A

A - augmented
B - bizarre
C - chronic
D - delayed
E - withdrawal or end of use
F - failure

22
Q

Drug-drug interaction drawbacks

A
  • increased toxicity
  • reduced efficacy
  • inconvenience
  • increased cost
23
Q

Drug-drug interactions benefits

A
  • reduced toxicity
  • increased efficacy
  • increased convenience
24
Q

Ca, Mg, iron containing foods effect on tetracycline

A

Inhibits oral absorption

25
Vitamin K effect on warfarin
Counteracting effect; may precipitate thrombosis
26
Cheese syndrome
MAO inhibitors prevent breakdown of tyramine from cheese
27
Grapefruit juice's bioflavonoids contain CYP450 inhibitors that reduce metabolism of...
- H1 blockers - Statins - Calcium channel blockers - Itraconazole - Amiodarone
28
Drug-herb interactions
- St. John's wort induces CYP450, interacts with multiple drugs - Gingko & ginseng reduce platelet aggregation & enhance risk of bleeding by Aspirin & Warfarin
29
Acetylcholine sites
- All preganglionic sites - All postganglionic parasympathetic endings - Sympathetic to sweat gland - Motor nerve endings in skeletal muscles
30
Noradrenaline sites
All postganglionic sympathetic nerve endings EXCEPT sweat glands
31
Noradrenaline & Adrenaline site
Adrenal medulla
32
Dopamine site
Renal vasculature
33
Alpha 1 antagonist CVS effect
vasodialtion ↓ peripheral resistance ↓ blood pressure ADR: MAY CAUSE POSTURAL HYPOTENSION
34
Alpha 2 antagonist CVS effect
↑ sympathetic outflow tachycardia
35
Alpha blockers effects:
- facilitate insulin release - facilitate miosis - nasal stuffiness - ejaculation failure - ↓ smooth muscle tone in prostate & bladder neck; ↓ resistance to urine outflow in BPH
36
Beta blockers bring about an antihypertensive effect by:
↓ heart rate ↓ contractility ↓ cardiac output ↓ renin release ↓ TPR (long-term)
37
Beta blockers bring about an antiarrhythmic effect by:
↓ sinus rate ↓ ectopic pacemaker activity ↓ conduction (membrane stabilization)
38
Beta blockers bring an anti-ischemic effect by:
↓ cardiac work ↓ oxygen demand
39
Beta blockers help in congestive cardiac failure by:
reducing sympathetic tone OD CAN WORSEN CCF
40
Autacoids classes
Amines - histamine, serotonin Lipids (Eicosanoids) - leukotriene B4, prostaglandin I2 Peptide - angiotensin, bradykinin
41
PGE1 analogues
- Misoprostol: prevent NSAID induced peptic ulcer & treatment of peptic ulcer - Alprostadil: treatment of erectile dysfunction
42
PGE2 analogues
Dinoprostone: include abortion & labor induction (cervical ripening)
43
PGEF2α analogues
Latanoprost: glaucoma treatment
44
Histamine H1 receptors
- smooth muscle, endothelial cells - causes acute allergic responses & inflammation
45
Histamine H2 receptors
- gastric parietal cells - increased secretion of gastric acid
46
Histamine H3 receptors
- central nervous system - modulating neurotransmission
47
H1 antihistamine: Diphenhydramine (gen1)
- cross BBB - short-acting (4-6 hours) - blocks muscarinic & α-adrenergic receptors
48
H1 antihistamine: Cetirizine, Loratadine (gen2)
- do not cross BBB (peripheral H1 binding only) - long-acting (12-24 hours) - selective to H1 receptors only
49
1st gen antihistamine ADR
- CNS depression - orthostatic hypotension - anticholinergic effects: dry mouth, urinary retention, blurred vision
50
2nd gen antihistamine ADR
- CNS depression minor risk - inhibit CYP450 increases QT interval; risk for arrhythmia (terfenadine)
51
1st gen antihistamine clinical use
- acute allergic reactions - motion sickness - morning sickness - vertigo - antitussives (cough med)
52
2nd gen antihistamine clinical use
- allergic rhinitis (hay fever) - allergic conjunctivitis (chronic allergic conditions)