Anti-Hypertensives Flashcards

1
Q

Dry mouth; sedation; rebound hypertension (on withdrawal)

A

Clonidine

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2
Q

Reflex tachycardia; Postural hypotension

A

Prazosin; Doxazosin

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3
Q

Sedation; postural hypotension (in volume depleted patients)

A

Methyldopa (Aldomet)

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4
Q

Therapy for hypertension during pregnancy

A

Methyldopa (Aldomet);

Clonidine

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5
Q

Used mainly in men with hypertension plus BPH

A

Prazosin; Doxazosin

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6
Q

βAdrenoceptor antagonists

Non-selective (competitively blocks β1 + β2 adrenoceptors)

(i) βBlockers (via β1) → ↓HR & ↓CO → ↓BP
(ii) β1Blockade → ↓Renin release
(iii) Blockade of β autoreceptors → ↓Sympathetic tone

A

Propranolol

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7
Q

– Dry cough
– Angioedema
– Teratogenic
Hyperkalemia

A

Captopril, Lisinopril, Enalapril, Ramipril

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8
Q

Do not enhance dilator effects of bradykinin

A

AT1- Receptor antagonists

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9
Q

β-Antagonists with Vasodilator Activities

β1 blocker + Vasodilation due to ↑Endothelial Nitric oxide (NO) release

Racemic mixture

D‐isomer → highly selective β1‐blocker;
L‐isomer → Vasodilation via ↑NO release

A

Nebivolol

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10
Q

– Hyperkalemia
– Renal impairment
– Potential teratogen

A

Aliskiren

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11
Q

(i) Reflex tachycardia;
(ii) Fluid retention;
(iii) Excessive hair growth;
(iv) Headaches/Flushing
excess cerebral/cutaneous dilation

A

Minoxidil; Pinacidil

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12
Q

↓Renin release (Kidney):
– ↓Angiotensin II/↓Arteriolar resistance
– ↓Aldosterone → ↓Na+ retention & ↓Blood volume

A

β blockers

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13
Q

a peripheral arteriolar dilator via agonist action at D1 receptors

A

Fenoldopam

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14
Q

Absorbed incompletely from the GIT;

Hardly cross the blood‐brain‐barrier

A

Hydrophilic β blockers

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15
Q

↓Ang. II & Aldosterone secretion; Dilates via ↓in Bradykinin breakdown or Increase in bradykinin secretions

A

Captopril, Lisinopril, Enalapril, Ramipril

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16
Q

Angioedema; teratogenic

A

Losartan, Candesartan, Valsartan, Eprosartan

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17
Q

AT1- Receptor antagonists

Blocks Angiotensin II actions at AT1 Receptors → ↓Vasoconstriction and ↓Aldosterone effects

A

Losartan, Candesartan, Valsartan, Eprosartan

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18
Q

Blood pressure (B.P.) =

A

C.O. x P.R.

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19
Q

bradycardia & cardiac conduction problems; impotence, peripheral vascular insufficiency, hyperglycemia, diabetes, asthma

Withdrawal s/s
nervousness, tachycardia, increase BP

A

Propranolol

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20
Q

Cardiac output (C.O) depends on

A

Stroke Volume (SV) & Heart Rate (HR)

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21
Q

Centrally‐acting sympatholytics

preferential α2 agonist stimulates
central presynaptic α2 adrenergic receptors →
↓Peripheral sympathetic drive via ↓NE release

A

Clonidine

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22
Q

Centrally‐acting sympatholytics
prodrug for methylnorepinephrine

Forms αmethylNE (an α2-agonist)
Central α2-agonism → ↓ Sympathetic tone

A

Methyldopa (Aldomet)

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23
Q

chemically‐related to thiazides but has no diuretic activity

Opens K+ channels → Hyperpolarization & prolonged dilation

  • Long‐lasting arteriolar dilation → rapid fall in systemic vascular resistance and fall in BP
  • Extensively bound to serum albumin & to vascular tissue; Dilates via the opening of K+ channels
A

Diazoxide

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24
Q

Contraindicated in asthma patients

Not effective in African American patients
Avoid nonselective blockers in COPD patients

A

Propranolol

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25
dilates arterioles but not veins
Hydralazine
26
Drug accumulate in patients with ↓hepatic blood flow, e.g., elderly, liver cirrhosis, & congestive heart failure
Lipophilic β blockers
27
Effectively treats hypertension, particularly in the elderly
Nifedipine; Amlodipine; Verapamil; Diltiazem
28
Elimination T1/2 = 1‐5 h
Lipophilic β blockers
29
Elimination T1/2: ↑ when GFR is ↓, e.g., | elderly, renal insufficiency
Hydrophilic β blockers
30
excessive lowering of BP; accumulation of cyanide byproduct of its metabolism
Sodium nitroprusside
31
Excreted unchanged or as active | metabolites by the kidney
Hydrophilic β blockers
32
Extensive metabolism in gut wall & the liver (1st pass effect) → Low oral bioavailability (10‐30%)
Lipophilic β blockers
33
extensively metabolized; excreted in urine [Tó = 6 h; Dosed once/day; ↓Renal function → ↓Dose]
Atenolol
34
Heart Rate (HR) depends on
sympathetic & parasympathetic | activities
35
Hydrophilic β blockers
Atenolol, Esmolol, Labetolol, | Carteolol, Nadolol
36
hypertension in pregnancy, & hypertension due to phaechromocytoma
Labetolol
37
Hypotension Peripheral edema Headache/dizziness
Nifedipine; Amlodipine
38
Hypotension Peripheral edema Headache/dizziness Cardiodepression
Verapamil; Diltiazem
39
KATP channel activators Selectively dilate arterioles via increases in K+ efflux through KATP channels Opens K+ channels → VSM hyperpolarization & relaxation
Minoxidil; Pinacidil
40
L-Type Ca2+ channel Blockers Dihydropyridines (DHPs): Greater block of vascular versus cardiac Ca2+ channels Relax VSM cells by inhibiting voltage-gated Ca2+ entry into cytosol
Nifedipine; Amlodipine
41
L-Type Ca2+ channel Blockers equi-active on heart & blood vessels Relax VSM cells by inhibiting voltage-gated Ca2+ entry into cytosol
Verapamil; Diltiazem
42
Lipophilic β blockers
Propranolol, Metoprolol , Pindolol, | Timolol
43
management of hypertensive emergency; administered with diuretic
Sodium nitroprusside Hydralazine Fenoldopam Diazoxide
44
metabolized by | hepatic CYP2D6; T1/2 = 4‐6 h
Metoprolol (β1‐selective)
45
Metabolized rapidly by RBC esterases; T1/2 = 9‐10 min, given by constant IV infusion
Esmolol (β1 blocker)
46
Modulation of central sympathetic drive to the | periphery
Lipophilic β‐blockers, e.g., propranolol
47
More effective blocker of RAS than ACE inhibitors
AT1- Receptor antagonists
48
nitric oxide donor → Dilation of both arteries & veins Activates soluble guanylate cyclase (sGC) → ↑Cellular cGMP & VSM cell relaxation & ↓BP
Sodium nitroprusside
49
No changes to Cardiac output, serum glucose or lipids
ACE Inhibitors
50
Peripheral Resistance (PR) determined by?
arteriolar tone
51
Peripheral α‐Adrenoceptor Blockers Selective αblockade → Arterial dilation
Prazosin; Doxazosin
52
Preferred in hypertensive diabetic patients (delay the onset/progression of diabetic renal damage)
Captopril, Lisinopril, Enalapril, Ramipril
53
Contraindication: PREGNANCY
Captopril, Lisinopril, Enalapril, Ramipril; Losartan, Candesartan, Valsartan, Eprosartan; Aliskiren
54
Primarily to treat severe or intractable | hypertension
Minoxidil; Pinacidil
55
Purpose(s) of Poly‐therapy
``` 1. Synergy of efficacy Vasodilators → Na+ retention & ↑Sympathetic activity (SA) Diuretics & β‐blockers → ↑Na+ excretion & ↓HR via SA node 2. Enhance long‐term beneficial effect ACE inhibitors (ACEIs) prevent renal damage in Stage 2 HPT patients; ACEI → ≈10 mmHg ↓BP 3. Toxicity prevents use of max. dose in mono‐therapy ```
56
Rapidly, completely absorbed in GIT; easy | entry to CNS → Central side effects
Lipophilic β blockers
57
Reflex sympathetic activation → Tachycardia; ↓Insulin release (due to Kchannel opening); Edema (salt and water retention)
Diazoxide
58
Reflex tachycardia; headache, flushing & ↑Intraocular pressure
Fenoldopam
59
Renin inhibitors Inhibits the enzyme activity of Renin – ↓Angiotensin I and Angiotensin II formation – ↓Aldosterone production and activity
Aliskiren
60
Stroke Volume (SV) depends on:
Plasma volume & Venous return
61
Sympathetic nerve terminal blockers adrenergic amine release blocker
Guanadrel
62
T1/2 = 6‐24 h; No interaction with liver metabolized | drugs
Hydrophilic β blockers
63
Useful in hypertensive patients with predisposition to, or with asthma, diabetes, or peripheral vascular disease
Metoprolol
64
VMAT; Vesicular monoamine transporter blocker Sympathetic nerve terminal blockers
Reserpine
65
β-Antagonists with Intrinsic Sympathomimetic Activity (Partial agonists; stimulates as well as blocks β-receptors) ↓Vascular resistance; ↓Cardiac output, & ↓Heart rate → ↓BP
Pindolol
66
β-Antagonists with Vasodilator Activities α1- + β-adrenergic blockade has 3:1 ratio of β:α antagonism after oral dosing
Labetolol
67
β-Antagonists with Vasodilator Activities β2-agonism + β-adrenergic blockade
Celiprolol
68
β1-Selective (Cardio-selective; β1 receptors predominate in the heart)
Metoprolol
69
β2 Agonist activity > β2 Antagonist activity, thus beneficial in treatment of Peripheral Vascular Disease
Pindolol