Drugs used for treatment of Hypertension 2 Flashcards
List the chemical derivates for selective CCB with mainly vascular effects
Dihydropyridine derivates
List the drugs for selective CCB with mainly vascular effects
Drug name
Amlodipine*
Felodipine
Lecanidipine
Nifedipine*
Nimodipine
list the chemical derivates for selective CCB with direct cardiac effects
Phenylalkylamine derivates
Benzothiazepine derivates
List the drugs for phenylalkylamine derivates
Verapimil
List the drugs for Benzothiazepine derivates
Diltiazem
explain the MoA of Calcium channel blockers
L-type calcium channels
Block cellular entry of Ca2+,through calcium channels rather than
preventing its intracellular actions
Many calcium channel antagonist show properties of?
Many calcium channel antagonists show properties of:
* Use dependence, the most active calcium channels are more
effectively blocked
* Voltage-dependent blocking, blocking is stronger when the
membrane is depolarised, causing calcium channel opening and
inactivation
explain the cardiac action for calcium channel blockers: physiological actions
Cardiac actions
* Cardio-selective: Verapamil
(diltiazem intermediate
selectivity)
* Antiarrhythmic affects (AV block
and cardiac slowing)
* Negative ionotropic effect
(contra-indicated in CCF)
Explain what calcium channel blockers do on vascular smooth muscle
Vascular smooth muscle
* Selective for smooth muscle:
Dihydropyridines – amlodipine
* Reflex tachycardia due to
vasodilator action
* Reduce blood pressure
* Can be used in CCF
* Coronary vasodilation use in
variant angina (cause by
vasospasm)
* Other smooth muscles are also
relaxed: biliary, urinary, uterine
Inidcation for calcium channel blockers
Hypertension: shown beneficial effects on cardiovascular morbidity
and mortality
explain the pharmacokinectis for calcium channel blockers
- Mostly given oral with good bioavailability, iv , e.g. nimodipine for
special indication (subarachnoid haemorrhage) - Extensively metabolised
- Amlodipine long elimination half-life (once daily dosing)
- Nifedipine, verapamil, diltiazem, short half-lives (formulations for
once daily dosing available)
What are adverse effects for short acting dihydrpyridine
Headache and flushing
list the adverse effects for chronic use of CCB
ankle swelling (pedal oedema) – vasodilation and
increased permeability
List adverse effects of verapamil
constipation, heart block, worsening heart failure
Name 2 classes of low-ceiling diuretics
Thiazides
Excluding thiazides