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PHARMACOLOGY > ANTIHYPERTENSIVES 1.0 > Flashcards

ANTIHYPERTENSIVES 1.0 Flashcards

1
Q

Give the classification of antihypertensive drugs

A

Diuretics
Sympatholytic drugs
Calcium channel blockers
Drugs acting on RAAS
Vasodilators

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2
Q

Give the Sympatholytic agents for hypertension

A

1) Alpha receptor antagonists
2) Beta receptor antagonists
3) Mixed beta and alpha receptor antagonists
4) Centrally acting adrenergic receptor agents
5) Adrenergic neuron blocking agents

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3
Q

Give the centrally acting receptor agonists

A

Methyldopa
Clonidine
Guanabenz
Guanfacine

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4
Q

Give the mechanism of action of the centrally acting antihypertensive agents

A

They act on a2 receptors in the brainstem for sympathetic inhibition by inhibiting release of NE

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5
Q

What is the function of the a2 receptors

A

When stimulated they inhibit NE release through feedback mechanism

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6
Q

What type of G protein coupled receptor is a2 receptor

A

Gi

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7
Q

Methyldopa is termed as a prodrug , explain

A

Methyldopa is converted to its active form methylnorepinephrine that works to stimulate the a2 receptors in the brainstem thus inhibiting NE release

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8
Q

Give five PK of methyldopa

A

1) Taken orally
2) Rapidly absorbed
3) Metabolized in the brain
4) Half life of two hours
5) Excreted in urine as sulfate conjugate(50-70%) and parent drug (25%)

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9
Q

Give uses of Methyldopa

A

Used as a hypertensive drug in pregnancy

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10
Q

Give the A/E of methyldopa

A

Dry mouth , Sedation , Hemolytic anemia (discontinue) , Positive Coombs test , Thrombocytopenia , Leukopenia , Red cell Aplasia , Prolactinemia , Parkinsonism

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11
Q

Clonidine is said to have two a2 receptor effects , give them

A

A2a stimulation in brainstem to reduce NE release
A2b stimulation in bloodvessels to bring vasoconstriction (high doses)

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12
Q

Clonidine reduces blood pressure by reducing the CO and PVR ,Explain

A

BP = CO X PVR
Clonidine reduces the CO in supine by
Reducing the HR , Stroke volume and myocardial contractility
It reduces the PVR in postural position

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13
Q

Reduction in the Myocardial contractility of Clonidine can predispose a patient to

A

Congestive Heart failure

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14
Q

Give atleast 10 A/E of Clonidine

A

sedation , dry mouth, nose and eyes , Erectile dysfunction , vivid dreams , depression , restlessness , sinus arrest , postural hypotension

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15
Q

To treat the withdrawl that comes fro sudden discontinuation , three things can be done?

A

1) Restore the drugs
2) Give sodium nitroprusside
3) Hive mixed alpha and beta blockers

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16
Q

Sudden discontinuation of Clonidine can lead to withdrawl effects such as

A

Headaches , Tremors , Apprehension , Abdominal pain , Tachycardia , Rebound hypertension

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17
Q

Clonidine is rarely used for hypertension. Give an important use of Clonidine.

A

Diagnosis of Phaeochromocytoma

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18
Q

Give two main Adrenergic blocking agents

A

Reserpine and Guanethidine

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19
Q

Give the mechanism of action of Guanethidine

A

Transported into the presynaptic membrane by NET transporters and stored in the NE vesicles thus deplets NE stores

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20
Q

Give the mechanism of action of Guanethidine

A

Transported into the presynaptic membrane by NET transporters and stored in the NE vesicles thus deplets NE stores

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21
Q

NET is inhibited by

A

Cocaine , Amphetamine, Tricyclic antidepressants , Phenoxybenzamine

22
Q

Give the PK of Guanethidine

A

Has a long half life of 5 days
Gradual onset of sympathoplegia with maximal effect in 2 weeks
Persisiting sympathoplegia even after cessation
Titrate dose of drug in 2week interval

23
Q

Give four A/E of Guanethidine

A

1) Postural hypotension
2) Retrograde ejaculation
3) Diarrhea
4) Hypertensive crisis in pheochromocytoma

24
Q

Give two main DDI in Guanethidine

A

Sympathomimetic agents - worsen hypertension
Tricyclic antidepressants

25
Q

Give the MOA of reserpine

A

Irreversibly Blocks the vessicle associated membrane transporter thus depletion of NE, serotonin and dopamine stores

26
Q

Give A/E of Reserpine

A

Severe depression ( discontinue)
Sedation
Nightmares
Parkinsonism
Postural hypotension
GIT problems

27
Q

Alpha receptor antagonists may be grouped into 3

A

1) Non selective
2) Selective
3) Ergot alkaloids

28
Q

Give the non-selective alpha receptor antagonists.

A

PPUTY
Phenoxybenzamine
Phentolamine
Urapidil
Tolazoline
Yohimbine

29
Q

Give the non-selective alpha receptor antagonists preferrentials

A

Phenoxybenzamine - a1 more than a2
Phentolamine - a1=a2
Urapidil - a1 more than a2
Tolazoline and Yohimbine - a2 more than a1

30
Q

Give the selective alpha receptor antagonists

A

PTTD
Prazosin , Terazosin , Trimazosin , Doxasozin
TA
Tamsulosin and Alfuzosin

31
Q

Give the types of beta receptor antagonists

A

1) Non-selective
2) Selective
3) Combined

32
Q

Give the none selective beta blockers

A

Propranolol
Pindolol
Timolol

33
Q

Give examples of selective beta blockers

A

b1 - Metoprolol, Betaxolol ,bisprolol ,atenolol, acebutolol, Tolamolol
b2 - butoxamine

34
Q

Give the mixed alpha and beta receptor antagonists

A

Labetolol
Carvedilol

35
Q

Give the MOA of Phenoxybenzamine

A

Irreversibly blocks alpha adrenoreceptors and thus reduce vasoconstriction cause by norepinehrine and epinenphrine

36
Q

What is the main clinical use of phenoxybenzamine

A

Pre and intra operative management of pheochromocytoma

37
Q

Give the A/E of phenoxybenzamine

A

Postural hypotension
Dry mouth
Inhibiton of ejaculation
Nasal stuffiness
Miosis

38
Q

Give three absolute C/I of Phenoxybenzamine

A

Porphyria
Hypovolemic states
History of cerebrovascular accidents

39
Q

Give relative C/I of phenoxybenzamine

A

Elderly patients
Pregnancy
Renal imparement
Marked arterioscleorsis

40
Q

ACE inhibitors have 2 main types of moa

A

1) Prevent conversion of Angiotensin I to II which is a potent vasocntrictor
2) Inhibits breakdown of bradykinin thus causes its accumulation and an increase in nitric oxide and prostacyclin which are potent vasodilator

41
Q

ACE inhibitors have 2 main types of moa

A

1) Prevent conversion of Angiotensin I to II which is a potent vasocntrictor
2) Inhibits breakdown of bradykinin thus causes its accumulation and an increase in nitric oxide and prostacyclin which are potent vasodilator

42
Q

ACE inhibitors are used in which type of hypertensive pateints

A

Patients with co morbidities such as diabetes ,

43
Q

All ACE inhibitors are guven orally except

A

Enalaprilat

44
Q

All ACE inhibitors are eliminated by the kidneys except

A

Fosinopril

45
Q

All ACEIs undego hepatic metabolism to active metabolites except

A

Captopril and Lisinopril

46
Q

ACEIs adverse effects include

A

Dry cough , rash , fever , altered taste , hypotension and hyperkalemia

47
Q

What rare but life threatening A/E may be associated with ACEIs

A

Angioedemea

48
Q

Which two things must be monitored in patients using ACE inhibitors

A

1) Potassium
2) Serum creatinie

49
Q

Give two examples of ARBs

A

Losartan and irbersartan

50
Q

ARBs are similar to ACE inhibitors but differ in one of the mechanisms

A

ARBs do not increase bradykinin levels

51
Q

Give a C/I for ACE inhibitors and ARBs

A

Pregnancy - teratogenic

52
Q

Give the three main classes of drug sas RAAS modulators and examples

A

1) ACE inhibitors - Lisinopril , Etanapril
2) ARBs - Losartan ,
3) Direct Renin inhibitors - Aliskerin

PHARMACOLOGY (17 decks)

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