Dihydropiridines: (selectively acts on coronary, arterioles) -they bind EC portion of Ca ch Alpha-1 subunit - short acting (T1/2= 6 hrs) : Nifedipine, Nimodipin - moderate (T1/2= 8-20 hr) : Felodipine, Nitredipin, nisoldipin long acting (T1/2= 35-50 hr) Amlodipine, Manidipin (has duiretic action, inhibit Na, H2o resorption) Non: (act in heart, coronary, arterioles) -Bind inner cytoplasmic part of alpha1 subunit Verapamil, Diltiazem -NEVER combine with BB bcz cardiac dep, AV block

B: 17-20 Flashcards by M AAB

Ca2+ ch. blockers

Dihydropiridines: (selectively acts on coronary, arterioles)
-they bind EC portion of Ca ch Alpha-1 subunit

short acting (T1/2= 6 hrs) : Nifedipine, Nimodipin
moderate (T1/2= 8-20 hr) : Felodipine, Nitredipin, nisoldipin

long acting (T1/2= 35-50 hr)
Amlodipine,
Manidipin (has duiretic action, inhibit Na, H2o resorption)

Non: (act in heart, coronary, arterioles)
-Bind inner cytoplasmic part of alpha1 subunit

Verapamil, Diltiazem

-NEVER combine with BB bcz cardiac dep, AV block

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Dihydropiridines

Nifedipine
Amlodipine
Felodipine
Nimodipine

-they bind EC portion of Ca ch Alpha-1 subunit

vascular >> cardiac effect

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Dihydropiridines indications

HTN
Angina
Arrythmias
Prinzmetal’s angina= vasospastic angina
Peripheral vascular disease
-Subarachnoid hemorrhage (Nimodipine)

Hypertensive emergency
Pregnancy HTN (Nifedipine)
Raynaud’s phenomenom

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Which drug should wew give in case of Subarachnoid hemorrhage

Nimodipine

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Verapamil indications

HTN
Angina (atherosclerotic , vasospastic)
Migrane prophylaxis
Anti arrhythmic class IV: AV node arrhythmia

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NO releasing agents

Hydralazine

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Hydralazine MOA, adminstration, duration

Induce release of NO from endothelial cells
Mainly arterial vasodil.
Orally active
6-8 h duration

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Hydralazine indications

HTN
used in combo with isosorbide dinitrate in heart failure

Induces baroreceptor homeostatic compensatory response; must use w duiretic OR BB

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Patient with HF and reduced ejection fraction can be given

Hydralazine + Isosorbide dinitrate

reduce mortality due to heart failure in African Americans.

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Hydralazine side effects

Drug induced Lupus at high dose
Tachycardia
Na, H2o retension

causes baro-r homeostatic response ; must be combined with diuretic or BB

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Endothelin antagonist

Bosentan

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Bosentan indications

Pulmonary HTN

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Bosentan side effects

Teratogenic
Hepatotoxicity

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PDE-5 inhibitor

Sildenafil

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Sildenafil indications

Erectile dysfunction
Pulmonary HTN

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Sildenafil side effects

Severe hypotension in combination with Nitrates
Priapism (Prolonges erection)
Blue tinted vision

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K sparing diuretics- Aldosteron-R inhibitors

Spironolactone
Eplerenone

steroid inhibitors of cytoplasmic Aldosterone-R in Cortical CD

Spironolactone . eplerenone duration of action

24-72 h

Spironolactone indications

Hyperaldestronism (primary conns disease, + secondary due to chronic HF , or hepatic cirrhosis)

Hypokalemia caused by other diuretics

Antiadronergic

Spironolactone side effects

Hyperkalemic metabolic acidosis (decreases exc of K, H ). (increase exc of Na

Anti-adronergic effect (gynecomastia w/ spironolactone use only)

ACE inhibitors MOA

Inhbition of ACE → ↓ AG-II, ↓ Aldosterone
↑ endogenous vasodilators (Bradykinin)

acts on both arterial and venous ; effectively reduces BP

ACE inhibitors names

Captopril
Enalapril
Perindopril
Ramipril

ACE inhibitors indications

HTN
Diabetic nephropathy
Chronic HF (reduced mortality)

Acute coronary syndrome

ACE inhibitors side effects

Dry cough
Teratogenic
Hyperkalemia
AKI in renal patients

ARB's

Losartan Valsartan Irbesartan

ARB's indications

HTN Protective of diabetes nephropathy CHF (reduced mortality) like ACE-I

ARB's side effects

Teratogenic Hyperkalemia

Drug used in Ischemic heart disease (Angina pectoris)

Nitroglycerine Isosorbid-mononitrate / dinitrate CCB B blockers (Propranonlol) Ivabradine (inhibit pacemaker If Na channel in SA node) Trimetazidine (pFOX inhibitor)- inhibit late Na channel in myocardium Ranolazine (pFOX inhibitor= partial fatty acid oxidation inhibitor ) - inhibit late Na channel in myocardium

Nitrates MOA

Release NO in smooth m NO stimulates guanylyl cyclase Increased in cGMP Dephosphorylation of myosin light chain Smooth muscle relaxation

Nitrates effects

Vasodilation (venous\>\>\>arterial) Preload ↓↓ Afterload ↓ Cardiac work ↓ O2 demand ↓

Short acting nitrates How to give Onset of action Duration of acation Indications

Nitroglycerin Sublingual Onset in 1 min Lasts 10-20 min **Acute angina, pectoris** **Acute coronary syndrome** ,Hypertensive emergency, Acute pulmonary edema

Intermediate acting nitrates How to give Onset of action Duration of acation Indications

Nitroglycerin (also isosorbide mononitrate in oral form) Oral Slow onset 2-4 h Angina prophylaxis Reduced mortalilty in atients with stable angina

Long acting nitrates How to give Onset of action Duration of acation Indications

Nitroglycerin Transdermal patch Slow 10 h Angina prophylaxis Reduced mortalilty in atients with stable angina

Isosorbid-dinitrate Evrything

Sublingual short acting rapidly denitrated in liver, smooth m to isosorbide mononitrate 20-30 min duration of action Acute angina pectoris Acute coronary syndrome Hypertensive emergency, Acute pulmonary edema

Nitrates side effects

Headache Reflex tachycardia Cutaneous flushing Orthostatic hypotension Syncope Methemoglobinemia in prolonged high dosage. (rxn with rbc) Tolerance after 8-10 h; INTERMITTENT treatment !!

Nitrates contraindications

Systolic BP \< 90 mmHg Right vent. MI (makes it worse because they act on venous side more!!) Patient took PDE-5 within last 24 h (synergistic relaxation of vascular s.m -\> dangerous hypotension, inadequate perfusion to critical organs) Hypertrophic obstructive cardiomyopathy

CCB used to treat angina

Nifedipine Verapamil Diltiazem

B blocker used in angina prophylaxis

Propranolol

L type Ca channel location

* cardiac * skeletal * smooth m * neurons * endocrine cells * bone Blocked by verapamil, DHP long, large threshold current

T type Ca channel location

heart neurons

N-type Ca channel location

* neuron * sperm (also R-type Ca channel inhibited by Gaba-pentin

pFOX inhibitors

**Trimetazidine** (pFOX inhibitor)- inhibit late Na channel in myocardium Ranolazine (pFOX inhibitor= partial fatty acid oxidation inhibitor ) - inhibit late Na channel in myocardium increase efficiency of O2 utilization by shifting heart preferance from fatty acid to glucose. SE: QT prolongation