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Sympathetic Depressants Flashcards

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1
Q

Adrenergic blockers

A

Alpha adrenergic(block N.A but reverse Adr because N.A has weak beta)
Beta adrenergic
Both

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2
Q

Non selective alpha blockers (receptors on bv so VD)

A

Ergot alkaloids(no vaso dilation)- ergo tamine, toxine(partial agonist for alpha and serotonin), metrine
Imidazoline derivatives - tolazoline and phentolamine
Betahaloalkylamine - phenoxybenzamine and dibenamine

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3
Q

Selective alpha 1 blockers

A

Pra(first dose phenomenon - postural hypotension with the first dose) trima tera doxa zosin and indoramine
*trima and indoramine show no first dose
*tera, doxa and tamsulosin are long acting

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4
Q

Selective alpha 2 blockers

A

Yohimbine (research)3356

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5
Q

Prazosin works through posts synaptic alpha blocking as well as what for VD

A

Phosphodiesterase increasing CAMP decreasing Ca so VD

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6
Q

Is there accompanied reflex tachycardia in VD caused he prazosin

A

Noi
It’s selective for alpha 1
It increases both CGMP (drop HR) and CAMP (raise HR)
So no significant change in HR

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7
Q

Prazosin VDs both arteries and veins

A

So Decreases both preload and afterload
Suitable for heart failure
Also used in hypertension when taken orally

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8
Q

There’s postural hypotension with which drug

A

Prazosin
First dose phenomenon (trimazosin and indoramine don’t)
Tera , doxa and tamsulosin are long acting

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9
Q

Beta blockers (compete with isoprenaline and block beta effect on adrenaline)

A

Divided according to solubility and selectivity

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10
Q

Non selective

A

*Propranolol lipophilic - no intilrinsic sympathetic activity and 95%bound
*Nadolol hydrophilic
Oxprenolol
Pindolol
Sotalol - lipophilic
On the eye: Timolol - hydrophilic
Betaxolol
Levobunolol
Carteolol
Pindolol and oxprenolol have all the ISA

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11
Q

Selective beta 1 more than 2

A

Metoprolol lipophilic -HF
* Atenolol hydrophilic
Practolol
Acebutolol
* Bisoprolol hydrophilic - HF
* Nebivolol hydrophilic - HF
Esmolol lipophilic

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12
Q

Selective beta 2

A

Butoxamine

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13
Q

Blocks beta and alpha 1

A

Labetalol
* Carvedilol - HF
Medroxalol
Bucindolol
**prizidilol

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14
Q

Nadolol, atenolol, sotalol

A

Excreted unchanged in urine so contraindicated in renal disease

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15
Q

Augments hypertensive effect but blocks bronchodilator effect of adrenaline

A

Propanolol

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16
Q

Beta blockers with vaso D properties

A

Blockers with partial agonist activity - celiprolol, dilecalol and nebivAlol
Additional VD molecule - carvedilol, labetolol, medroxalol, bucindolol and prizidilol
Potent antihypertensive for peripheral vascular diseases and heart failure

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17
Q

Interfering with adrenergic release

A

Guanthedine

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18
Q

Interfering with adrenergic storage

A

Reserpine

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19
Q

Interfering with adrenergic synthesis

A

Alpha methyl dopa

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20
Q

Presynaptic alpha 2 stimulator(inhibitory)

A

Clonidine
Guanfacine and alpha methyl dopa
Imidazoline receptors agonists- rilmendine and moxonidine

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21
Q

According to solubility

A

Lipophilic pass bbb and have sedation side effects, depression and night mare plus hepatic first oass for 4 to 6hours
Hydrophilic doesn’t pass bbb and lasts 12 to 24 hours

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22
Q

Give sildenafil(viagra)

A

Orally on empty stomach 1hr before intercourse

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23
Q

Decrease in aqueous humour caused by

A

Beta blocker(propranolol)effect on the eye decreasing IOP

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24
Q

Class 2 antiarrhythmic action of beta blockers

A

Beta blockade
Sodium channel blocker
Quinidine like action
Local anaesthetic action

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25
Inhibiting beta 1 in the kidney
Decreases renin decreasing BP
26
Hypoglycemia in beta blockers
Block beta 2 on liver
27
Atherosclerosis in beta blockade
B3 inhibition and decrease HDL
28
Propranolol on CVS * give orally or slow IV
Angina prophylaxis Acute MI - antiarrhythmic action plus blocks K uptake so reduces work and size of infarction Arrhythmia after Sympathomimetics, thyrotoxicosis and digitalis Hypertrophic Obstructive Cardiomyopathy BV Aortic Aneurysm and varices in liver cirrhosis as it decreases COP and splanchnic circulation BP hypertension
29
Pheochromocytoma
Tumor in adrenal gland Treated by alpha and beta blockers
30
Loss of selectivity of beta blockers
In large doses
31
ISA Drugs under VD properties
Celiprolol Dilevalol Nebivalol
32
Therapeutic alpha uses
Hypertension with excess catechos Primary Hypertension PVD Reverse VC by leakage of NA during infusion Benign prostatic hyperplasia Benign prostatic hyperplasia- no Contractions e.g prazosin and doxazosin
33
First pass in propranolol so
2/3 lost to liver (there's glucoronic acid conjugation) and 1/3 in systematic circulation -some are not bound and excreted unchanged in urine so renal disease contraindication
34
Propranolol Bbb so used as
Antiparkinsonian Antianxiety Plus prophylaxis in migraine
35
Most important effect of BB - CVS
Decreases chrono ino AV conduction cardiac work Oxygen
36
Effect of BB on BP
Presynaptic effect decreasing sympathetic and NA release On heart Kidney Rest barorwceptir sensitivity PG, VD BB, Decreased TPR - BV action
37
Blocks hypotensive Isoprenaline and Beta stinukant
Propranolol
38
Antagonizes bronchodilatkr Adr
May precipitate asthmatics
39
Beta blockers in angina
Decreases work of the heart plus BPplus anxiety so used in stable A but NOT in VARIANT as alpha is left unopposed so VC which may worsen the condition
40
Beta blockers in MI
Reduces the work of the heart plus size of infarct Antiarrhythmic action Hypokalemic action
41
With selective beta blocker, you're less liable yo side effects
Less Reynaud's phenomenon Less Bronchospasm Less Hypoglycemia Less lipotropic changes Less hypokalemia
42
Beta blockers in HF (moderate)
Prevent toxic catechos Blocks RAS Decreases incidenc of sudden death and increases survival in post infarction patients -beta 1 more than 2 (affects heart more than bv)
43
Side Effects (SE)
In severe depression use hydrophilic BB
44
SE BB on heart
HB and HF Not used with variant angina(worsens) Not with verapamil abd diltiazem
45
SE BB on BV
Reynauds Cold extremities Numbness - so not used in PVD plus reynauds
46
SE BB BP
Hypotension
47
SE BB respiration
Bronchial asthma
48
Sudden discontinuation of BB
Sympathetic overactivity With angina and MI
49
Special drugs at the end
SDATE
50
Non selective mention sdate
PNST
51
Nadolol *sdate*
Angina HT once a day
52
Sotalol *sdate*
Class 3 antiarrhythmic
53
Timolol *sdate*
In open angle glaucoma as eye drop Avoided in heart block(it's still a beta blocker) Doesn't affect size of pupil (does nothing for accommodation) as it decreases aqueous humor directly
54
Selective B mentioned at the end
MABEN
55
Nadolol
Atenolol
56
Metoprolol = Esmolol = Propranolol
Angina Arrhythmia Hypertension
57
Esmolol
Metabolised by blood esterase in liver Ultra short half life - 10 minutes In supraventricular arrhythmia and severe hypertension Given IV
58
Nebivolol
Most B1 selective N = NO for VD May increase insulin sensitivity and doesn't affect lipid profile
59
Beta and Alpha - Labetalol 3:1
No selective B so doesn't affect CO and no ISA Quick drop on BP because alpha and renin No tachycardia
60
More labetalol - uses
Hypertension- IV in severe hypertension Pheochromocytoma * Carvedilol is also an antioxidant Plus Medroxalol, and bucindolol exist
61
Antiadrenergic drugs
Adrenergic neuron blockers
62
Inhibit release
Guanthedine
63
Inhibit synthesis
Alpha methyl dopa
64
Reserperine
Inhibit storage plus mentioned under Tyramine
65
Alpha 2 agonists - centrally acting
Stimulates presynaptic alpha 2 in: Brain stem - Decreased sympathetic flow Kidney- Decreased renin Nerve endings- Decreased NA Plus decreased renal vascular resistance so hypertension with renal insufficiency

Pharmacology (29 decks)

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