II. Mechanism

  1. Cellular channel effects
    1. Effects slow Calcium channel activity (blocks voltage-gated L-type Calcium channels)
    2. Agents block both Calcium and Sodium inflow into cells during smooth muscle Action Potential phase
    3. Channels are present in cardiac and vascular Smooth Muscle
  2. Calcium Channel Blocker effects
    1. Myocardial relaxation (Non-Dihydropyridines primarily)
    2. Vascular Smooth Muscle relaxation
    3. Pancreatic B-islet cell inhibition
    4. Inhibits gastrointestinal Smooth Muscle propulsion (resulting in Constipation)

III. Types

  1. Dihydropyridine (e.g. Nifedipine, Amlodipine)
    1. Primary effects are on peripheral vasculature, resulting in vasodilation (with possible reflex increased Heart Rate)
    2. Amlodipine (Norvasc) is most commonly used and typically for Hypertension
    3. Nicardipine and Clevidipine are most commonly used in Hypertensive Emergency
  2. Non-Dihydropiridine (e.g. Verapamil, Diltiazem)
    1. Effect both peripheral vasculature and cardiac tissue, with a decrease in Heart Rate and Blood Pressure
    2. Diltiazem is most commonly used and typically used for Atrial Fibrillation Rate Control

IV. Adverse Effects: Myocardial Infarction

  1. Short Acting Calcium Channel Blockers
    1. Findings
      1. Myocardial Infarction Risk: 60% over Diuretics
      2. Higher dose confers >3x risk of lower dose
    2. References
      1. Psaty (1995) JAMA 274:620-5, 654-5 [PubMed]
      2. Furberg (1995) Circulation 92: 1326-31, 1068-73 [PubMed]
  2. Long acting Calcium Channel Blockers
    1. No increased cardiovascular disease risk
    2. Reference
      1. Alderman (1997) Lancet 349:594-8 [PubMed]

V. Adverse Effects: Bleeding risk

  1. Findings
    1. Higher Incidence of GI Hemorrhage in elderly
    2. Associated with Platelet aggregation inhibition
    3. Avoid in older patients if:
      1. Peptic Ulcer Disease
      2. Concurrent Aspirin use
      3. Perioperative
  2. References
    1. Pahor M (1996) Lancet 347:1061-5 [PubMed]
    2. Wagenknecht (1995) BMJ 310(6982):776-7 [PubMed]
    3. Zuccala (1997) BMJ 314:643-4 [PubMed]

VI. Adverse Effects: General

  1. Hypotension
  2. Flushing
  3. Nasal congestion
  4. Tachycardia
  5. Dizziness
  6. Nausea
  7. Nervousness
  8. Bowel changes
  9. Gingival Hyperplasia
  10. Eczematous Dermatitis (or other skin reactions)
    1. Occurs in up to 1% of patients on Calcium Channel Blockers
    2. Delayed onset at 3 months after starting Calcium Channel Blockers
    3. Joly (2007) J Invest Dermatol 127(12):2766-71 [PubMed]

VII. References

  1. (2022) Presc Lett 29(11): 64-5
  2. Yen (2015) Crit Dec Emerg Med 29(10): 18-23

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Ontology: Calcium Channel Blockers (C0006684)

Definition (MSH) A class of drugs that act by selective inhibition of calcium influx through cellular membranes.
Definition (CSP) class of drugs that act by selective inhibition of calcium influx through cell membranes or on the release and binding of calcium in intracellular pools; since they are inducers of vascular and other smooth muscle relaxation, they are used in the drug therapy of hypertension and cerebrovascular spasms, as myocardial protective agents, and in the relaxation of uterine spasms.
Concepts Pharmacologic Substance (T121)
MSH D002121
SnomedCT 372245007, 48698004, 373304005
LNC LP31438-2
English Blockers, Calcium Channel, Channel Blockers, Calcium, Calcium Channel Blocking Drugs, CHANNEL BLOCK CA, CA CHANNEL BLOCK, calcium antagonist, calcium channel blocking agents, calcium channel blockers (medication), calcium channel blockers, [CV200] CALCIUM CHANNEL BLOCKERS, Calcium channel blockers, calcium channel blocker, agents blocking calcium channel, calcium-channel blocker, calcium channel blocking agent, CALCIUM CHANNEL BLOCKERS, Calcium channel blocker (product), Calcium--Antagonists, Antagonists, Calcium Channel, Calcium Channel Antagonists, Calcium-channel blocker, Calcium channel blocker (substance), Calcium channel blocker, Calcium channel blocking agent (product), Calcium channel blocking agent, Calcium channel blocking agent, NOS, Calcium channel blocking agent (substance), Calcium Channel Blockers, Calcium Channel Blocker, Calcium Channel Blocking Agents
French Bloqueurs des canaux calcium, Bloqueurs des canaux du calcium, Inhibiteurs des canaux du calcium, Inhibiteurs des canaux calciques, Inhibiteurs des canaux calciques exogènes, Antagonistes calciques exogènes, Inhibiteurs des canaux calcium, Antagonistes calciques, Bloqueurs des canaux calciques exogènes, Inhibiteurs calciques
Swedish Kalciumkanalblockerare
Spanish antagonista del calcio, Bloqueantes de los Canales de Calcio, bloqueante de los canales de calcio, bloqueante de los canales de calcio (producto), agente bloqueante de canal de calcio (producto), agente bloqueante de canal de calcio, antagonista del calcio (producto), antagonista del calcio (sustancia), bloqueante de los canales del calcio (sustancia), bloqueante de los canales del calcio, Bloqueadores de los Canales de Calcio, Antagonistas Exógenos del Calcio, Bloqueadores Exógenos del Calcio, Inhibidores Exógenos del Calcio
Czech exogenní antagonisté vápníku, vápníkové kanály - blokátory, blokátory kalciových kanálů, blokátory kalciového kanálu, blokátory vápníkových kanálů
Finnish Kalsiuminestäjät
Italian Esogeni bloccanti del calcio, Esogeni calcio-antagonisti, Esogeni inibitori del calcio, Sostanze bloccanti del canale del calcio, Bloccanti del canale del calcio
Russian KAL'TSIIA BLOKATORY EKZOGENNYE, KAL'TSIIA INGIBITORY EKZOGENNYE, KAL'TSIEVYKH KANALOV BLOKATORY, KANALOV KAL'TSIEVYKH BLOKATORY, KAL'TSIIA ANTAGONISTY EKZOGENNYE, BLOKATORY KAL'TSIEVYKH KANALOV, БЛОКАТОРЫ КАЛЬЦИЕВЫХ КАНАЛОВ, КАЛЬЦИЕВЫХ КАНАЛОВ БЛОКАТОРЫ, КАЛЬЦИЯ АНТАГОНИСТЫ ЭКЗОГЕННЫЕ, КАЛЬЦИЯ БЛОКАТОРЫ ЭКЗОГЕННЫЕ, КАЛЬЦИЯ ИНГИБИТОРЫ ЭКЗОГЕННЫЕ, КАНАЛОВ КАЛЬЦИЕВЫХ БЛОКАТОРЫ
Japanese カルシウム拮抗剤, カルシウムチャネル遮断剤, カルシウムチャネルブロッカー, カルシウムチャンネルブロッカ, カルシウムチャンネルブロッカー, カルシウム拮抗薬, 外因性カルシウム抑制薬, 外因性カルシウム拮抗薬, 外因性カルシウム遮断薬, カルシウムチャンネル遮断剤, カルシウム遮断薬
Croatian KALCIJ, ANTAGONISTI
Polish Blokery kanałów wapniowych, Inhibitory kanałów wapniowych
German Calciumantagonisten, exogene, Calciumblocker, exogene, Calciuminhibitoren, exogene, Calciumkanalblocker, Kalziumantagonisten, exogene, Kalziumblocker, Kanalblocker, Calcium-, Kalziumantagonisten
Portuguese Antagonistas Exógenos do Cálcio, Bloqueadores dos Canais de Cálcio, Bloqueadores Exógenos do Cálcio, Inibidores Exógenos do Cálcio