Antihypertensives

Question 1

Desirable blood pressure?

Answer 1

115/75 or lower

Question 2

Hypertensive urgency values

Answer 2

220/120

Question 3

Secondary hypertension

Answer 3

We know what causes hypertension (5-10%) cocaine and oral contraceptives (increase BP) pheochromocytoma-tumor of adrenal gland

Question 4

Primary hypertension

Answer 4

Cause is unknown

Question 5

Malignant HT

Answer 5

220/120 or higher

Question 6

Why hypertension kills

Answer 6

Stroke

MI

Left ventricular hypertrophy

Aneurysm

Renal failure

Question 7

What controls our BP when we sit up suddenly

Answer 7

Neuronal-vascular control loop

Question 8

What does Ca influx into vessels cause?

Answer 8

Contraction

Question 9

What does K efflux into vessels cause?

Answer 9

Relaxation

Question 10

Increase in cGMP in vessels causes?

Answer 10

Contraction

Question 11

What does angiotensin II on vessels cause?

Answer 11

Contraction

Question 12

What does DA influx into vessels cause?

Answer 12

Relaxation

Question 13

What does endothelin receptor on vessels cause?

Answer 13

Contraction

Question 14

When BP or Na levels in the kidney drop what happens

Answer 14

Renin is secreted

Question 15

What controls our BP long term?

Answer 15

Kidney control loop (renin-angiotensin-aldosterone system)

Question 16

What does renin do?

Answer 16

Angiotensinogen–>A1

Question 17

What converts A1–>A2

Answer 17

Angiotensin converting enzyme (ACE)

Question 18

What does ACE do?

Answer 18

A1–>A2

Bradykinin–>inactive product

Question 19

What does bradykinin do?

Answer 19

Dilates arteries (drops BP)

Capillary leakage (edema) Activates sensory nerves-pain and itching

Question 20

What does A2 do?

Answer 20

Vasoconstriction

Na retention

Aldosterone

Question 21

One SE of all antihypertensives

Answer 21

Hypotension

Question 22

Alpha-methyl DOPA

Answer 22

Central alpha-2 agonist

Prodrug: metabolized to alpha-methyl NE

SE:

Depression

Drowsiness

Dry mouth

Impaired Ejac.

Hepatic dysfunction

Question 23

Clonidine

Answer 23

Central alpha-2 agonist

SE:

Depression

Drowsiness

Dry mouth

Impaired Ejac.

Unlabeled uses:

• Fibromyalgia-unspecified neuronal pain
• Insomnia
• Tourettes
• Opiate withdrawal

Question 24

Propranolol

Answer 24

Tx of hypertension

Nonselective Beta blocker

Central and peripheral effects

Mech:

• Blocks B1 receptors on heart, prevents rise in HR
• Decreases renin secretion
  
  • Renin converts Angiotensinogen→A1

SE:

• Into CNS→Depression
• Bradycardia→fatigue
• Impotence
• Lowers HDL, raises triglycerides
• Exacerbates asthma

Question 25

Reserpine

Answer 25

Tx of HT Central and peripheral effects/effector of post-ganglionic neuron Causes depletion of post ganglionic neuron nt (NE)→ No vasoconstriction SE: depression, drowsiness, diarrhea

Question 26

alpha-methyl tyrosine

Answer 26

Tx of pheochromocytoma Central and peripheral effects Inhibits tyrosine kinase--preventing synthesis NE and epi

Question 27

"Osin"s

Answer 27

Alpha 1 blockers Blocks alpha 1 receptor on vascular smooth m Tx of hypertension and some specifically treat BPH Based on the drugs he gave us: \*\*If it ends in -azosin its for hypertension\*\* \*\*If it ends in just -osin its used for BPH\*\* SE * First dose effect-rapid drop in BP→orthostatic (postural) hypotension * Do not confuse w/ first pass effect

Question 28

More selective B blockers

Answer 28

Metoprolol Acebutolol Atenolol Betaxolol Nebivolol SE: * Fewer CNS effects * Bradycardia * Fatigue w/ exercise

Question 29

Combined alpha and beta blockers

Answer 29

Block alpha1, beta1, and beta2 Labetalol Carvedilol SE: * Postural hypotension * Dry mouth

Question 30

Angiotensin receptor blockers

Answer 30

"-Artan"s SE: * Decrease secretion of aldosterone * Fetal abnormalities * All agents that alter angiotensin system * Pregnancy risk X

Question 31

Endothelin blockers

Answer 31

"-entan"s Tx of pulmonary arterial hypertension SE: * Fetal damage * Testicular atrophy * Hepatic toxicity

Question 32

Minoxidil

Answer 32

*Acts directly on smooth muscle* Prodrug Opens K channels in arterial smooth m, increased efflux→hyperpolarization Very refractory px SE: * Hypertrichosis-hair growth * Rogaine * Discontinuation→hair loss * Edema and pericardial effusion→cardiac tamponade * Fluid in sac around heart

Question 33

Hydralazine

Answer 33

*Act directly on smooth muscle* Arterial vasodilator Increase in cGMP→relaxes smooth m SE: * Slow acetylators→lupus like syndrome

Question 34

Diazoxide

Answer 34

*Acts directly on smooth muscle* Opens K channels→hyperpolarization SE: * Decreased insulin secretion from beta cells in pancreas→hypoglycemia

Question 35

Nitroprusside

Answer 35

*Acts directly on smooth muscle* Drug of choice in hypertensive emergencies Acts w/in seconds--given IV Dilates art and veins→drop in BP increases cGMP→relaxation Rapidly degrades in soln into cyanide

Question 36

Calcium channel blockers

Answer 36

"-ipine"s Inhibit Ca influx into vascular smooth m Prevent vasoconstriction SE: * Heartburn * May worsen heart failure

Question 37

ACE inhibitors

Answer 37

"-pril"s ACE responsible for A1→A2 ACE responsible for bradykinin breakdown Leads to decreased aldosterone secretion SE: * Rash * Dry cough that cant be treated with suppressants * Angioneurotic edema-swelling of nose, throat, resp tract * Taste alteration * Fetal damage

Question 38

Aliskiren

Answer 38

Renin inhibitor SE: * Fetal damage * Diarrhea * Cough * Angioedema

Question 39

Fenoldopam

Answer 39

Activate D1 receptors Given IV for HT emergencies