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Pharma S1Y2 > alpha and beta blockers + sympatholytics > Flashcards

alpha and beta blockers + sympatholytics Flashcards

1
Q

whats the function of alpha 1 receptors ?

A

1- effect on vessels =VASOCONSTRICTION

2- effect on uterus : Contraction

3- eyes : vasoconstriction of the muscles leading to dilated pupils

4- wall of GIT/BLADDER = dilation

5- splinchter GIT/BLADDER = contraction ( if alpha is blocked lead to urine retention )

6- sweat glands of the palm and forehead = sweating

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2
Q

what is the function of alpha 2 receptors?

A

its mainly presynaptic :

it has inhibitory effect —-> inhibit the release of noreephrine –> relaxation and vasodilation

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3
Q

whats the function of alpha blocker?

A

1- vasodilation MOST important
and the opposite of everything mentioned in the function

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4
Q

what reflex does do alpha blockers do?

A

reflex tachycardia due to hypotension because they cant reset the baroreceptor like ace and bb

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5
Q

what are the 2 types of alpha blockers? give examples

A

non selective which block both alpha 1 and alpha 2 like ( AMINE ):

phenoxybenzamine
Phentolamine

Selective alpha 1 blockers ( OSIN) :

Prazosin- PROTOTYPE
Doxazosin
Terazosin

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6
Q

why dont we have selective alpha 2 blockers?

A

cuz alpha 2 is a good receptor and it causes inhibition and relaxations

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7
Q

what are the uses of non selective alpha blockers? phenoxybenzamine/phentolamine

A

is no longer used for hypertension but it is used for PHEOCHROMACYTOMA

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8
Q

what are the uses of selective alpha blockers ? prazosin doxazoin terazosin

A

there are 3 uses :

1- HYPERTENSION

2- PHEOCHROMOCYTOMA in combination with beta blocker (b4 surgery)

3- TREATMENT OF RAYNAUD DISEASE ( which ischemia due to vasoconstriction, you give alpha blocker cuz it causes vasodilation )

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9
Q

whats happens when you give the first dose alpha blockers? But its resolved later when body adjusts to it

A

SEVERE hypotension and syncope + reflex tachycardia

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10
Q

what is the function of beta 1 receptors?

A

In heart : Increases all aspects of the heart : contractility ,cardiac output, heart rate, everything

in kidneys : Release of renin

Vessels : Vasodilation

Lipolysis

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11
Q

whats the function of beta 2 receptors?

A

نصف الرجوله b2
In skeletal muscle :
1- Vasodilation = more blood to muscles
2- Increase sensitivity of muscles
3- takes potassium from blood and take it to the muscle –> hypokalemia

In liver : glycolysis you need energy for running

in trachea : bronchodilation you need air to run

In eyes : increase the aqueous humor to increase the eye pressure –> when you are running theres pressure in your eyes the aqueous humor will counter this pressure – > beta blockers can be used in glucoma

in heart : Vasodilation of coronary arteries —> beta agonist can be used in angina and prinzemetal angina

-Utertine : relaxation -when you are running and you are pregnant you dont want to contract w gg

In CNS : release norepinephrine

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12
Q

whats the function of beta blockers?

A

the antihypertensive effects :

1- Decrease cardiac output ( due to blockage b1 decreasing heart rate )

2- decrease sympathetic flow from CNS ( Due to blockage of b2 )

3- Inhibit renin release ( due to blockage of b2 )

4-increase PGI and nitiric oxide leading to vasodilation

5- reset baroreceptor no tachycardia like ACE

6-bronchoconstriction – contraindicated in asthma patients

7- inhibit glycogenlysis in liver

and opposite of everything else mentioned before

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13
Q

what are the types of beta blockers and give examples

A

non selective beta blockers block both beta 1 and beta 2 :

Propranol = the prototype
Nodalol
Timolol
pindolol
penbutalol
Cartelol

selective beta blockers block beta 1 only :

metaprolol
Atenolol
acebutalol
bisoprolol
nebivolol

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14
Q

whats the different functions of both types?

A

the none selective, block both b1 and b2 leading to:
decrease HR and contractility
decrease renin release
vasodilation
decrease cns sympathetic activity
inhibit glycogenlysis
bronchoconstriction

But the selective ones only work on heart and kidney and vessels

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15
Q

which beta blocker has extended period of action?

A

nadolol non selective

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16
Q

which beta blocker causes vasodilation by nitric oxide release

A

nebivolol selective

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17
Q

which beta blockers require dosage reduction in renal failure

A

nadolol and cartelol both are none selective

18
Q

which beta blocker is used in glucoma

A

timolol ( non selective ) and betaxolol

19
Q

which beta blockers are cardio selective

A

atenolol and metaprolol both are selective

20
Q

which beta blocker are lipophilic and metabolized in liver

A

PM
proprolol and metaprolol

21
Q

which beta blockers are lipophobic and excreted unchanged in urine

A

AS
atenolol and sotalol

22
Q

what is the most selective beta blocker

A

nebivolol

23
Q

what are the adverse effects of beta blocker?

A

1- hear failure cuz heart depressing
2- bradycardia no reflex tachycardia cuz they reset baroreceptor
3-heart block from depressing
4- bronchoconstriction
5- sedation
6- sudden stop , if you want to stop , stop gradually to avoid arrhythmia and hypertension

24
Q

what are the contraindication of beta blocker

A

1- asthma patients cuz bronchoconstriction

2- prinzemetal angina ( you should beta agonist not antagonist )
3- peripheral vascular disease ( RAYNAUD FOR EXAMPLE, peripheral vascular disease means ischemia , you dont want to give bb cuz you need beta vasodilation effect )

4- alone in pheochromocytoma

be caution in diabetes patients cuz sometimes sugar drops and when bb are used it will inhibit glycogenlysis and there wont be sugar to help., this is most likely avoided when using selective cuz selective inhibit b1 alone and not b2 and b2 is responsible for glycogenlysis

25
Q

how is bb administered ?

A

orally, iv

26
Q

what are drugs that inhibit both alpha and beta receptor together

A

labetalol and carvedilol

27
Q

how is labetalol administered

A

IV and orally

Labetalol is used in emergencies cuz its IV

28
Q

whats the special point of labetalol and carvedilol

A

they can be used alone in pheochromocytoma cuz they block both a and b

29
Q

is labetalol and carvedilol safe for pregnancy?

A

yes both can be used

30
Q

what reflex does labetalol cause

A

it doesnt cause any reflex and not reflex tachycardia cuz its also a beta blocker and it reset baroreceptor

31
Q

whats the difference between labetalol and carvedilol

A

carvedilol has greater b blockage effect compared to labetalol

32
Q

what are centrally acting sympatholytic

A

drugs that are alpha 2 agonists

33
Q

what are the functions of sympatholytic

A

they activate alpha 2 receptors in the brain which inhibit noreepinephrine and and lead to relaxation

34
Q

what are the 2 examples of sympatholytics

A

alpha methyl dopa

clonidine

35
Q

what are the adverse effects of methyl dopa

A

hemolytic anemia

36
Q

whats the best scenario where you use clonidine/methyl

A

hypertension + renal failure

37
Q

what is clonidine usually administered with and how its administered

A

its given with diuretics cuz it causes water sodium retention

its administered IV, Orally, Patch

38
Q

what are the adverse effects of clonidine ?

A

Sedation
Drying of nasal mucosa

39
Q

what happens when you stop suddenly?

A

rebound hypertension js like beta blockers so you must stop slowly and gradually

40
Q

what do you give with vasodilators ?

A

diuretics and bb cuz vasodilators lead to reflex tachycardia and increased renin release + water retention
you give diuretics and to counter the water retention and bb to counter reflex tachycardia

41
Q

what are the drugs safe for pregancy until now

A

number 1 always :-

1- ALPHA METHYL DOPA /Clonidine
2- labetalol/carvedilol

42
Q

what are the drugs that can be used for emergencies until now

A

1- enalaprilat iv
2- labetalol IV

Pharma S1Y2 (6 decks)

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