Pharmacology: hypertension and antihypertensives (major drugs) Flashcards
What are some risk factors for CVD?
Sex (male)
Age (older)
Smoking
Diabetes
Cholesterol
Systolic BP
Define normotensive and hypertensive in terms of systolic/diastolic BP
Normotensive: 90-140/60-90
Hypertensive: >140/>90
Hypertension may be primary (essential) or secondary. What does this mean?
Primary (essential): we don’t know the cause
Secondary: occurs secondarily to a disease (known cause)
Can hypertension be either symptomatic or asymptomatic?
Hypertension is a risk factor for _______ ___________ and _________.
Yes
Heart disease and stroke
5 non pharmacological means for managing hypertension?
Increase exercise
Decrease weight
Improve diet
Cease smoking
Limit alcohol intake
What are the 4 main types of antihypertensives?
ACE inhibitors
Angiotensin receptor blockers
Calcium channel blockers
Diuretics
ACE INHIBITORS
Mechanism of action?
Angiotensin converting enzyme (ACE) usually converts angiotensin I to angiotensin II; and bradykinin to junk products.
Angiotensin II usually leads to vasoconstriction and salt retention.
ACE inhibitors block the above processes –> inhibiting vasoconstriction and salt retention –> lowers BP, reduces hypertension.
ACE INHIBITORS
Indications (other than hypertension)
Heart failure, renoprotection in diabetes
ACE INHIBITORS
ADRs: cardiovascular
Hypotension
Oedema
Hyperkalemia (esp with preexisting renal impairment)
Compensatory tachycardia, palpitations, anginal pain
Headache
ACE INHIBITORS
ADRs: renal
Impairment
Bradykinin isn’t broken down as much –> dry cough
ACE INHIBITORS
ADRs: GI
Nausea
Vomiting
Abdominal pain
Taste disturbances
ACE INHIBITORS
ADRs: what are the elderly predisposed to? How to manage?
First dose hypotension (BP drops significantly on first dose, before returning) and hyperkalemia –> it’s important to start LOW doses at a SLOW pace in the elderly
ACE INHIBITORS
What two cases should ACE inhibitors be avoided in?
Bilateral artery stenosis (increased risk of renal failure)
Pregnancy (can harm developing fetus’ kidneys)
ACE INHIBITORS
Suffix?
Example?
What drug ends in this suffix but is NOT an ACE inhibitor?
-pril
Perindopril
Verapamil - a calcium channel blocker
ANGIOTENSIN RECEPTOR BLOCKERS
- MOA?
- Are its indications/contraindications/ADRs basically the same as ACE inhibitors? What is the one difference?
- Suffix and example?
Yes, however doesn’t affect bradykinin breakdown - less cough.
-sartan, eg. irbesartan
CALCIUM CHANNEL BLOCKERS
MOA:
- What channels do they block?
- What are their two classifications (location)?
L type (voltage gated) calcium channels
Central and peripheral
CALCIUM CHANNEL BLOCKERS
Peripheral: MOA?
Blocks these calcium channels.
Reduces calcium entry into vascular arteriolar SMCs
Causes arteriolar vasodilation –> relieves hypertension
CALCIUM CHANNEL BLOCKERS:
Peripheral: ADRs
GENERAL TO CENTRAL AND PERIPHERAL
Hypotension
Dizziness/syncope
Headache
Nausea
Diarrhoea
SPECIFIC TO PERIPHERAL
Oedema
Facial/neck flushing
CALCIUM CHANNEL BLOCKERS
Peripheral: examples
Dihydropyridines eg. amlodipine
CALCIUM CHANNEL BLOCKERS
Central: MOA?
Block L type (voltage gated) calcium channels in the heart. Reduces conduction, HR, and contractility
CALCIUM CHANNEL BLOCKERS
Central: contraindications?
Heart failure - further depresses heart function
Beta blockers - additive effect
CALCIUM CHANNEL BLOCKERS
Central: ADRs?
GENERAL TO CENTRAL AND PERIPHERAL
Hypotension
Dizziness/syncope
Headache
Nausea
Diarrhoea
SPECIFIC TO CENTRAL
Reduced myocardial workload
Bradycardia
Dysrhythmias
CALCIUM CHANNEL BLOCKERS
Central: examples?
Verapamil, diltiazem
CALCIUM CHANNEL BLOCKERS
Indications, in addition to hypertension?
Angina and tachydysrhythmias (especially central calcium channel blockers)
DIURETICS
MOA?
Increase sodium and water excretion from the kidney –> treat hypertension
Vasodilators at small doses
DIURETICS
ADRs: metabolic?
Electrolyte imbalances - hyponatremia, hypomagnesemia, hypokalemia, hypercalcemia, hyperuricemia
Hypercholesterolaemia
Glucose intolerance
Itchy skin (pruritis)
DIURETICS
ADRs: CVS + renal?
Dehyrdation
Hypotension, dizziness
Increased urinary frequency
DIURETICS
ADRs: other?
Erectile dysfunction
Loss of appetite
DIURETICS
Suffix?
Examples?
-ide
Eg. hydrochlorothiazide, indapamide
Drug escalation protocol?
Can drug resistant hypertension exist?
What % of patients does it occur in?
Yes
~10%