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Pharmacology part 3 > Calcium channel blockers > Flashcards

Calcium channel blockers Flashcards

1
Q

block sodium

A

lidocaine

-fast

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2
Q

block calcium

A

calcium channel blockers

-slow

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3
Q

calcium channel blockers

A
  • verapamil (phenylalkylamine)
  • diltiazem(benzothiazepine)
  • nifedipine (dihydropyridine)
  • all others CCB analogs of nifedipine
  • all block calcium channels
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4
Q

3 tissues calcium channel blockers act on

A
  1. myocardium
  2. AV node and conducting system
  3. blood vessels
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5
Q

myocardium CCB

A

verapamil +++
diltiazem ++
nifedipine 0/+

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6
Q

AV node and conducting system CCB

A

verapamil, diltiazem +++

nifedipine 0

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7
Q

blood vessels CCB

A

nifedipine +++
verapamil ++
diltiazem +

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8
Q

medical use of CCB

A
  1. atrial tachycardias (flutter, fib)
  2. stable angina
  3. prinzmetals angina
  4. hypertension
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9
Q

CCB use in: atrial tachycardias

A
  • blocks excess impulses coming through AV node and conducting system
  • diltiazem or verapamil used
  • nifedipine-type cause vasodilation and reflex tachycardia
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10
Q

CCB use in: stable angina

A

exercise related

  • diltiazem best ?
  • verapamil depressed heart too much
  • nifedipine type cases reflex tachycardia
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11
Q

CCB use in: prinzmetals angina

A

non-exercise related

  • best drugs for variant angina, all relax skeletal muscle
  • all CCB’s relax vasospams
  • blood vessels most affected: brain, heart, skeletal muscle
  • beta-blockers not very effective
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12
Q

CCB use in: hypertension

A
  • higher the blood pressure, greater the effect
  • good for all categories
  • beta-blockers not so good in elderly or in AA
  • CCBs more effect in elderly
  • no effect on blood lipids
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13
Q

CCB use in: threatened miscarriage

A
  • prematurity still major cause infant death
  • calcium channel in uterus
  • nifedipine effective
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14
Q

proposed use for CCB

A

Migraine
-verapamil some effect
-block initial vasospam
tried for prevention of 2nd heart attack

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15
Q

precautions in use of CCB’s

A
  1. most common complaint from vasodilation: dizziness, facial flush
    - decrease exercise tolerance verapamil, diltiazem
  2. constipation: elderly
  3. CNS effects: insomnia, nervousness, increase effect of morphine
  4. edema: dilate arteries not veins, increase capillary pressure (occurs in 11% of patients taking nifedipine)
  5. anti-platelet effect: bruising, petechiae (on hand), bleeding in peptic ulcer
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16
Q

what can short acting CCBs cause?

A

worsen angina and cause MI

-use amlodipine (half-life 39 hours)

17
Q

MOA of CCB

A
  • bind inside channel
  • different CCB act on different sites, explains lack os SAR
  • binding a function of voltage for nifedipine type
18
Q

why doesn’t nifedipine have an effect on the heart?

A
  • binding a function of voltage for nifedipine type
  • strong voltage fluctuations in heart displace drug-> not so in blood vessels
  • -voltage change causes decrease in affinity for receptor
19
Q

“use dependence” CCB means?

A
  • verapamil can get in only when channel opened electrically (use dependence)
  • diltiazem also somewhat use-dependent
  • explains why these drugs better when BP is high
  • nifedipine blocks right away, no need to depolarize
20
Q

when can nifedipine bind CC?

A

when calcium channel is inactive

  • not plugs
  • analog: Bay K 8644, open channels
21
Q

when can verapamil bind CC?

A

when calcium channel is open

-may be a plug

22
Q

binding sites for CCB

A
  • explains slow calcium entry

- explains ions selectivity

23
Q

new designation of Calcium channel: L

A

Ca1 family

-Ca 1.2 in heart and blood vessels

24
Q

new designation of Calcium channel: T

A

Ca3 family

  • regulate electrical excitability in many tissues
  • can enhance amplitude of depolarization in heart, neurons
25
Q

new designation of Calcium channel: P/Q, N

A

Ca2 family
-Ca 2.1-> P/Q purkinje
Ca 2.3-> N neuronal
-regulate neurotransmitter release in brain

26
Q

VSCC

A

mutlimeric proteins

-alpha-1 subunit forms the pore and contains drug binding sites

27
Q

functions of calcium channel subunits

A
  • alpha-2-gamma: cause faster opening/closing
  • beta: regulates trafficking alpha-1 to membrane, also allows more current after small depolarization
  • gamma: present in skeletal muscle channel but rarely elsewhere
28
Q

other CCB

A
  1. Magnesium
    - weak channel blocker
    - sometimes used in arrhythmias
  2. Hydrogen
    - strong competitor of calcium
    - but some drugs don’t work well at low pH
  3. older drugs: Barbiturates

Pharmacology part 3 (13 decks)

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