fbpx
Wikipedia

Diltiazem

August 27, 2023

Diltiazem, sold under the brand name Cardizem among others, is a calcium channel blocker medication used to treat high blood pressure, angina, and certain heart arrhythmias.[8] It may also be used in hyperthyroidism if beta blockers cannot be used.[8] It is taken by mouth or injection into a vein.[8] When given by injection, effects typically begin within a few minutes and last a few hours.[8]

Diltiazem
Clinical data
Pronunciation/dɪlˈtaɪəzɛm/
Trade namesCardizem, Dilacor XR, Cartia XT, others
AHFS/Drugs.comMonograph
MedlinePlusa684027
License data
Pregnancy
category
Routes of
administration		By mouth, intravenous
Drug classNondihydropyridine calcium channel blocker
ATC code
Legal status
Legal status
Pharmacokinetic data
Bioavailability40%
MetabolismLiver
Elimination half-life3–4.5 hours
ExcretionKidney
Bile duct
Identifiers
  • cis-(+)-[2-(2-Dimethylaminoethyl)-5-(4-methoxyphenyl)-3-oxo-6-thia-2-azabicyclo[5.4.0]undeca-7,9,11-trien-4-yl]ethanoate
CAS Number
  • 42399-41-7 Y
PubChem CID
  • 39186
IUPHAR/BPS
  • 2298
DrugBank
  • DB00343 Y
ChemSpider
  • 35850 Y
UNII
  • EE92BBP03H
KEGG
  • D07845 Y
ChEBI
  • CHEBI:101278 Y
ChEMBL
  • ChEMBL23 Y
PDB ligand
  • D6C (PDBe, RCSB PDB)
CompTox Dashboard (EPA)
  • DTXSID9022940
ECHA InfoCard100.050.707
Chemical and physical data
FormulaC22H26N2O4S
Molar mass414.52 g·mol−1
3D model (JSmol)
  • Interactive image
  • O=C2N(c3c(S[C@@H](c1ccc(OC)cc1)[C@H]2OC(=O)C)cccc3)CCN(C)C
  • InChI=1S/C22H26N2O4S/c1-15(25)28-20-21(16-9-11-17(27-4)12-10-16)29-19-8-6-5-7-18(19)24(22(20)26)14-13-23(2)3/h5-12,20-21H,13-14H2,1-4H3/t20-,21+/m1/s1 Y
  • Key:HSUGRBWQSSZJOP-RTWAWAEBSA-N Y
  (verify)

Common side effects include swelling, dizziness, headaches, and low blood pressure.[8] Other severe side effects include an overly slow heart beat, heart failure, liver problems, and allergic reactions.[8] Use is not recommended during pregnancy.[8] It is unclear if use when breastfeeding is safe.[1]

Diltiazem works by relaxing the smooth muscle in the walls of arteries, resulting in them opening and allowing blood to flow more easily.[8] Additionally, it acts on the heart to prolong the period until it can beat again.[9] It does this by blocking the entry of calcium into the cells of the heart and blood vessels.[10] It is a class IV antiarrhythmic.[11]

Diltiazem was approved for medical use in the United States in 1982.[8] It is available as a generic medication.[8] In 2020, it was the 76th most commonly prescribed medication in the United States, with more than 9 million prescriptions.[12][13] An extended release formulation is also available.[8][14]

Medical uses Edit

Diltiazem is indicated for:

For supraventricular tachycardias (PSVT), diltiazem appears to be as effective as verapamil in treating re-entrant supraventricular tachycardia.[17]

Atrial fibrillation[18] or atrial flutter is another indication. The initial bolus should be 0.25 mg/kg, intravenous (IV).

Because of its vasodilatory effects, diltiazem is useful for treating hypertension. Calcium channel blockers are well tolerated, and especially effective in treating low-renin hypertension.[19]

It is also used as topical application for anal fissures because it promotes healing due to its vasodilatory property.[20]

Contraindications and precautions Edit

Diltiazem is relatively contraindicated in the presence of sick sinus syndrome, atrioventricular node conduction disturbances, bradycardia, impaired left ventricle function, peripheral artery occlusive disease, and chronic obstructive pulmonary disease.

Side effects Edit

A reflex sympathetic response, caused by the peripheral dilation of vessels and the resulting drop in blood pressure, works to counteract the negative inotropic, chronotropic and dromotropic effects of diltiazem. Undesirable effects include hypotension, bradycardia, dizziness, flushing, fatigue, headaches and edema.[21] Rare side effects are congestive heart failure, myocardial infarction, and hepatotoxicity.[22]

Diltiazem is one of the most common drugs that cause drug-induced lupus, along with hydralazine, procainamide, isoniazid, minocycline.[23]

Drug interactions Edit

Because of its inhibition of hepatic cytochromes CYP3A4, CYP2C9 and CYP2D6, there are a number of drug interactions.[24] Some of the more important interactions are listed below.

Beta-blockers Edit

Intravenous diltiazem should be used with caution with beta-blockers because, while the combination is most potent at reducing heart rate, there are rare instances of dysrhythmia and AV node block.[25]

Quinidine Edit

Quinidine should not be used concurrently with calcium channel blockers because of reduced clearance of both drugs and potential pharmacodynamic effects at the SA and AV nodes.[26]

Fentanyl Edit

Concurrent use of fentanyl with diltiazem, or any other CYP3A4 inhibitors, as these medications decrease the breakdown of fentanyl and thus increase its effects.[27]

Mechanism Edit

 
180 mg Cardizem capsule

Diltiazem, also known as (2S,3S)-3-acetoxy-5-[2-(dimethylamino)ethyl]-2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one hydrochlorid has a vasodilating activity attributed to the (2S,3S)-isomer.[28] Diltiazem is a potent vasodilator, increasing blood flow and variably decreasing the heart rate via strong depression of A-V node conduction. It binds to the alpha-1 subunit of L-type calcium channels in a fashion somewhat similar to verapamil, another nondihydropyridine (non-DHP) calcium channel blocker.[29] Chemically, it is based upon a 1,4-thiazepine ring, making it a benzothiazepine-type calcium channel blocker.[citation needed]

It is a potent and mild vasodilator of coronary and peripheral vessels, respectively,[30] which reduces peripheral resistance and afterload, though not as potent as the dihydropyridine (DHP) calcium channel blockers. This results in minimal reflexive sympathetic changes.[citation needed]

Diltiazem has negative inotropic, chronotropic, and dromotropic effects. This means diltiazem causes a decrease in heart muscle contractility – how strong the beat is, lowering of heart rate – due to slowing of the sinoatrial node, and a slowing of conduction through the atrioventricular node – increasing the time needed for each beat. Each of these effects results in reduced oxygen consumption by the heart, reducing angina, typically unstable angina, symptoms. These effects also reduce blood pressure by causing less blood to be pumped out.

Research Edit

Diltiazem is prescribed off-label by doctors in the US for prophylaxis of cluster headaches. Some research on diltiazem and other calcium channel antagonists in the treatment and prophylaxis of migraine is ongoing.[15][31][32][33][34][35][36][needs update]

Recent research[when?] has shown diltiazem may reduce cocaine cravings in drug-addicted rats.[37] This is believed to be due to the effects of calcium blockers on dopaminergic and glutamatergic signaling in the brain.[38] Diltiazem also enhances the analgesic effect of morphine in animal tests, without increasing respiratory depression,[39] and reduces the development of tolerance.[40]

Diltiazem is also being used in the treatment of anal fissures. It can be taken orally or applied topically with increased effectiveness.[41] When applied topically, it is made into a cream form using either vaseline or Phlojel. Phlojel absorbs the diltiazem into the problem area better than the vaseline base. It has good short-term success rates.[42][43]

References Edit

  1. ^ a b "Diltiazem Use During Pregnancy". Drugs.com. 4 May 2020. Retrieved 5 May 2020.
  2. ^ . emc. 22 March 2018. Archived from the original on 28 August 2021. Retrieved 13 April 2020.
  3. ^ "Angitil SR/XL Capsules – Summary of Product Characteristics (SmPC)". (emc). 7 May 2019. Retrieved 13 April 2020.
  4. ^ "Cardizem- diltiazem hydrochloride tablet, coated". DailyMed. 2 June 2020. Retrieved 23 October 2022.
  5. ^ "Cardizem CD- diltiazem hydrochloride capsule, coated, extended release". DailyMed. 30 April 2020. Retrieved 23 October 2022.
  6. ^ "Cardizem LA- diltiazem hydrochloride tablet, extended release". DailyMed. 2 May 2019. Retrieved 23 October 2022.
  7. ^ "Active substance(s): diltiazem" (PDF). European Medicines Agency. 11 January 2018.
  8. ^ a b c d e f g h i j k "Diltiazem Hydrochloride Monograph for Professionals". Drugs.com. AHFS. Retrieved 28 December 2018.
  9. ^ Cardiovascular Pharmacotherapeutics. Cardiotext Publishing. 2011. pp. 251–52. ISBN 978-1935395621. Retrieved 28 December 2018.
  10. ^ 2010 Nurse's Drug Handbook. Jones & Bartlett Learning. 2010. p. 320. ISBN 978-0763779009.
  11. ^ Milne GW (2005). Gardner's Commercially Important Chemicals: Synonyms, Trade Names, and Properties. John Wiley & Sons. p. 223. ISBN 978-0471736615. Retrieved 28 December 2018.
  12. ^ "The Top 300 of 2020". ClinCalc. Retrieved 7 October 2022.
  13. ^ "Diltiazem – Drug Usage Statistics". ClinCalc. Retrieved 7 October 2022.
  14. ^ "Diltiazem hydrochloride – diltiazem hydrochloride extended-release tablets tablet, extended release". DailyMed. 1 April 2019. Retrieved 13 April 2020.
  15. ^ a b Grossman E, Messerli FH (2004). "Calcium antagonists". Progress in Cardiovascular Diseases. 47 (1): 34–57. doi:10.1016/j.pcad.2004.04.006. PMID 15517514.
  16. ^ Claas SA, Glasser SP (May 2005). "Long-acting diltiazem HCl for the chronotherapeutic treatment of hypertension and chronic stable angina pectoris". Expert Opinion on Pharmacotherapy. 6 (5): 765–776. doi:10.1517/14656566.6.5.765. PMID 15934903. S2CID 39272285.
  17. ^ Gabrielli A, Gallagher TJ, Caruso LJ, Bennett NT, Layon AJ (October 2001). "Diltiazem to treat sinus tachycardia in critically ill patients: a four-year experience". Critical Care Medicine. 29 (10): 1874–1879. doi:10.1097/00003246-200110000-00004. PMID 11588443. S2CID 25104288.
  18. ^ Wattanasuwan N, Khan IA, Mehta NJ, Arora P, Singh N, Vasavada BC, Sacchi TJ (February 2001). "Acute ventricular rate control in atrial fibrillation: IV combination of diltiazem and digoxin vs. IV diltiazem alone". Chest. 119 (2): 502–506. doi:10.1378/chest.119.2.502. PMID 11171729.
  19. ^ Basile J (November 2004). "The role of existing and newer calcium channel blockers in the treatment of hypertension". Journal of Clinical Hypertension. 6 (11): 621–629, quiz 630–631. doi:10.1111/j.1524-6175.2004.03683.x. PMC 8109670. PMID 15538095. S2CID 23440538.
  20. ^ Griffin N, Acheson AG, Jonas M, Scholefield JH (October 2002). "The role of topical diltiazem in the treatment of chronic anal fissures that have failed glyceryl trinitrate therapy". Colorectal Disease. 4 (6): 430–435. doi:10.1046/j.1463-1318.2002.00376.x. PMID 12790914. S2CID 32959944.
  21. ^ Ramoska EA, Spiller HA, Winter M, Borys D (February 1993). "A one-year evaluation of calcium channel blocker overdoses: toxicity and treatment". Annals of Emergency Medicine. 22 (2): 196–200. doi:10.1016/S0196-0644(05)80202-1. PMID 8427431.
  22. ^ Talreja O, Cassagnol M (2019). "Diltiazem". StatPearls. Treasure Island (FL): StatPearls Publishing. PMID 30422532.
  23. ^ Solhjoo M, Ho CH, Chauhan E (2019). "article-24529". Drug-Induced Lupus Erythematosus. Treasure Island (FL): StatPearls Publishing. PMID 28722919. Retrieved 20 November 2019.
  24. ^ Ohno Y, Hisaka A, Suzuki H (2007). "General framework for the quantitative prediction of CYP3A4-mediated oral drug interactions based on the AUC increase by coadministration of standard drugs". Clinical Pharmacokinetics. 46 (8): 681–696. doi:10.2165/00003088-200746080-00005. PMID 17655375. S2CID 41343222.
  25. ^ Edoute Y, Nagachandran P, Svirski B, Ben-Ami H (April 2000). "Cardiovascular adverse drug reaction associated with combined beta-adrenergic and calcium entry-blocking agents". Journal of Cardiovascular Pharmacology. 35 (4): 556–559. doi:10.1097/00005344-200004000-00007. PMID 10774785.
  26. ^ Narimatsu A, Taira N (August 1976). "Effects of atrio-ventricular conduction of calcium-antagonistic coronary vasodilators, local anaesthetics and quinidine injected into the posterior and the anterior septal artery of the atrio-ventricular node preparation of the dog". Naunyn-Schmiedeberg's Archives of Pharmacology. 294 (2): 169–177. doi:10.1007/bf00507850. PMID 1012337. S2CID 21986119.
  27. ^ . Archived from the original on 3 December 2017. Retrieved 26 June 2019.
  28. ^ Matsumae H, Akatsuka H, Shibatani T (2010). "Diltiazem Synthesis". Encyclopedia of Industrial Biotechnology. doi:10.1002/9780470054581.eib603. ISBN 978-0471799306.
  29. ^ O'Connor SE, Grosset A, Janiak P (1999). "The pharmacological basis and pathophysiological significance of the heart rate-lowering property of diltiazem". Fundamental & Clinical Pharmacology. 13 (2): 145–153. doi:10.1111/j.1472-8206.1999.tb00333.x. PMID 10226758. S2CID 20440286.
  30. ^ Gordon SG, Kittleson MD (2008). "Drugs used in the management of heart disease and cardiac arrhythmias". Small Animal Clinical Pharmacology. Elsevier. pp. 380–457. doi:10.1016/b978-070202858-8.50019-1. ISBN 978-0-7020-2858-8.
  31. ^ Montastruc JL, Senard JM (April 1992). "[Calcium channel blockers and prevention of migraine]" [Calcium channel blockers and prevention of migraine]. Pathologie-Biologie (in French). 40 (4): 381–388. PMID 1353873.
  32. ^ Kim KE (February 1991). "Comparative clinical pharmacology of calcium channel blockers". American Family Physician. 43 (2): 583–588. PMID 1990741.
  33. ^ Andersson KE, Vinge E (March 1990). "Beta-adrenoceptor blockers and calcium antagonists in the prophylaxis and treatment of migraine". Drugs. 39 (3): 355–373. doi:10.2165/00003495-199039030-00003. PMID 1970289. S2CID 13621196.
  34. ^ Paterna S, Martino SG, Campisi D, Cascio Ingurgio N, Marsala BA (July 1990). "[Evaluation of the effects of verapamil, flunarizine, diltiazem, nimodipine and placebo in the prevention of hemicrania. A double-blind randomized cross-over study]". La Clinica Terapeutica. 134 (2): 119–125. PMID 2147612.
  35. ^ Smith R, Schwartz A (May 1984). "Diltiazem prophylaxis in refractory migraine". The New England Journal of Medicine. 310 (20): 1327–1328. doi:10.1056/NEJM198405173102015. PMID 6144044.
  36. ^ Peroutka SJ (November 1983). "The pharmacology of calcium channel antagonists: a novel class of anti-migraine agents?". Headache. 23 (6): 278–283. doi:10.1111/j.1526-4610.1983.hed2306278.x. PMID 6358127. S2CID 40215836.
  37. ^ Common Heart Drug May Reduce Cocaine Cravings. Sciencedaily.com (28 February 2008). Retrieved on 2012-10-21.
  38. ^ Mills K, Ansah TA, Ali SF, Mukherjee S, Shockley DC (July 2007). "Augmented behavioral response and enhanced synaptosomal calcium transport induced by repeated cocaine administration are decreased by calcium channel blockers". Life Sciences. 81 (7): 600–608. doi:10.1016/j.lfs.2007.06.028. PMC 2765982. PMID 17689567.
  39. ^ Kishioka S, Ko MC, Woods JH (May 2000). "Diltiazem enhances the analgesic but not the respiratory depressant effects of morphine in rhesus monkeys". European Journal of Pharmacology. 397 (1): 85–92. doi:10.1016/S0014-2999(00)00248-X. PMID 10844102.
  40. ^ Verma V, Mediratta PK, Sharma KK (July 2001). "Potentiation of analgesia and reversal of tolerance to morphine by calcium channel blockers". Indian Journal of Experimental Biology. 39 (7): 636–642. PMID 12019755.
  41. ^ Jonas M, Neal KR, Abercrombie JF, Scholefield JH (August 2001). "A randomized trial of oral vs. topical diltiazem for chronic anal fissures". Diseases of the Colon and Rectum. 44 (8): 1074–1078. doi:10.1007/BF02234624. PMID 11535842. S2CID 40406260.
  42. ^ Nash GF, Kapoor K, Saeb-Parsy K, Kunanadam T, Dawson PM (November 2006). "The long-term results of diltiazem treatment for anal fissure". International Journal of Clinical Practice. 60 (11): 1411–1413. doi:10.1111/j.1742-1241.2006.00895.x. PMID 16911570. S2CID 23510129.
  43. ^ Sajid MS, Rimple J, Cheek E, Baig MK (January 2008). "The efficacy of diltiazem and glyceryltrinitrate for the medical management of chronic anal fissure: a meta-analysis". International Journal of Colorectal Disease. 23 (1): 1–6. doi:10.1007/s00384-007-0384-x. PMID 17846781. S2CID 13015745.

External links Edit

  • "Diltiazem". Drug Information Portal. U.S. National Library of Medicine.

August 27, 2023
diltiazem, sold, under, brand, name, cardizem, among, others, calcium, channel, blocker, medication, used, treat, high, blood, pressure, angina, certain, heart, arrhythmias, also, used, hyperthyroidism, beta, blockers, cannot, used, taken, mouth, injection, in. Diltiazem sold under the brand name Cardizem among others is a calcium channel blocker medication used to treat high blood pressure angina and certain heart arrhythmias 8 It may also be used in hyperthyroidism if beta blockers cannot be used 8 It is taken by mouth or injection into a vein 8 When given by injection effects typically begin within a few minutes and last a few hours 8 DiltiazemClinical dataPronunciation d ɪ l ˈ t aɪ e z ɛ m Trade namesCardizem Dilacor XR Cartia XT othersAHFS Drugs comMonographMedlinePlusa684027License dataUS DailyMed DiltiazemPregnancycategoryAU C 1 Routes ofadministrationBy mouth intravenousDrug classNondihydropyridine calcium channel blockerATC codeC05AE03 WHO C08DB01 WHO Legal statusLegal statusAU S4 Prescription only UK POM Prescription only 2 3 US only 4 5 6 EU Rx only 7 In general Prescription only Pharmacokinetic dataBioavailability40 MetabolismLiverElimination half life3 4 5 hoursExcretionKidneyBile ductIdentifiersIUPAC name cis 2 2 Dimethylaminoethyl 5 4 methoxyphenyl 3 oxo 6 thia 2 azabicyclo 5 4 0 undeca 7 9 11 trien 4 yl ethanoateCAS Number42399 41 7 YPubChem CID39186IUPHAR BPS2298DrugBankDB00343 YChemSpider35850 YUNIIEE92BBP03HKEGGD07845 YChEBICHEBI 101278 YChEMBLChEMBL23 YPDB ligandD6C PDBe RCSB PDB CompTox Dashboard EPA DTXSID9022940ECHA InfoCard100 050 707Chemical and physical dataFormulaC 22H 26N 2O 4SMolar mass414 52 g mol 13D model JSmol Interactive imageSMILES O C2N c3c S C H c1ccc OC cc1 C H 2OC O C cccc3 CCN C CInChI InChI 1S C22H26N2O4S c1 15 25 28 20 21 16 9 11 17 27 4 12 10 16 29 19 8 6 5 7 18 19 24 22 20 26 14 13 23 2 3 h5 12 20 21H 13 14H2 1 4H3 t20 21 m1 s1 YKey HSUGRBWQSSZJOP RTWAWAEBSA N Y verify Common side effects include swelling dizziness headaches and low blood pressure 8 Other severe side effects include an overly slow heart beat heart failure liver problems and allergic reactions 8 Use is not recommended during pregnancy 8 It is unclear if use when breastfeeding is safe 1 Diltiazem works by relaxing the smooth muscle in the walls of arteries resulting in them opening and allowing blood to flow more easily 8 Additionally it acts on the heart to prolong the period until it can beat again 9 It does this by blocking the entry of calcium into the cells of the heart and blood vessels 10 It is a class IV antiarrhythmic 11 Diltiazem was approved for medical use in the United States in 1982 8 It is available as a generic medication 8 In 2020 it was the 76th most commonly prescribed medication in the United States with more than 9 million prescriptions 12 13 An extended release formulation is also available 8 14 Contents 1 Medical uses 2 Contraindications and precautions 3 Side effects 4 Drug interactions 4 1 Beta blockers 4 2 Quinidine 4 3 Fentanyl 5 Mechanism 6 Research 7 References 8 External linksMedical uses EditDiltiazem is indicated for Stable angina exercise induced diltiazem increases coronary blood flow and decreases myocardial oxygen consumption secondary to decreased peripheral resistance heart rate and contractility 15 16 Variant angina it is effective owing to its direct effects on coronary dilation Unstable angina preinfarction crescendo diltiazem may be particularly effective if the underlying mechanism is vasospasm Myocardial bridgeFor supraventricular tachycardias PSVT diltiazem appears to be as effective as verapamil in treating re entrant supraventricular tachycardia 17 Atrial fibrillation 18 or atrial flutter is another indication The initial bolus should be 0 25 mg kg intravenous IV Because of its vasodilatory effects diltiazem is useful for treating hypertension Calcium channel blockers are well tolerated and especially effective in treating low renin hypertension 19 It is also used as topical application for anal fissures because it promotes healing due to its vasodilatory property 20 Contraindications and precautions EditIn congestive heart failure patients with reduced ventricular function may not be able to counteract the negative inotropic and chronotropic effects of diltiazem the result being an even higher compromise of function With SA node or AV conduction disturbances the use of diltiazem should be avoided in patients with SA or AV nodal abnormalities because of its negative chronotropic and dromotropic effects Low blood pressure patients with systolic blood pressures below 90 mm Hg should not be treated with diltiazem Diltiazem may paradoxically increase ventricular rate in patients with Wolff Parkinson White syndrome because of accessory conduction pathways Diltiazem is relatively contraindicated in the presence of sick sinus syndrome atrioventricular node conduction disturbances bradycardia impaired left ventricle function peripheral artery occlusive disease and chronic obstructive pulmonary disease Side effects EditA reflex sympathetic response caused by the peripheral dilation of vessels and the resulting drop in blood pressure works to counteract the negative inotropic chronotropic and dromotropic effects of diltiazem Undesirable effects include hypotension bradycardia dizziness flushing fatigue headaches and edema 21 Rare side effects are congestive heart failure myocardial infarction and hepatotoxicity 22 Diltiazem is one of the most common drugs that cause drug induced lupus along with hydralazine procainamide isoniazid minocycline 23 Drug interactions EditBecause of its inhibition of hepatic cytochromes CYP3A4 CYP2C9 and CYP2D6 there are a number of drug interactions 24 Some of the more important interactions are listed below Beta blockers Edit Intravenous diltiazem should be used with caution with beta blockers because while the combination is most potent at reducing heart rate there are rare instances of dysrhythmia and AV node block 25 Quinidine Edit Quinidine should not be used concurrently with calcium channel blockers because of reduced clearance of both drugs and potential pharmacodynamic effects at the SA and AV nodes 26 Fentanyl Edit Concurrent use of fentanyl with diltiazem or any other CYP3A4 inhibitors as these medications decrease the breakdown of fentanyl and thus increase its effects 27 Mechanism Edit 180 mg Cardizem capsuleDiltiazem also known as 2S 3S 3 acetoxy 5 2 dimethylamino ethyl 2 3 dihydro 2 4 methoxyphenyl 1 5 benzothiazepin 4 5H one hydrochlorid has a vasodilating activity attributed to the 2S 3S isomer 28 Diltiazem is a potent vasodilator increasing blood flow and variably decreasing the heart rate via strong depression of A V node conduction It binds to the alpha 1 subunit of L type calcium channels in a fashion somewhat similar to verapamil another nondihydropyridine non DHP calcium channel blocker 29 Chemically it is based upon a 1 4 thiazepine ring making it a benzothiazepine type calcium channel blocker citation needed It is a potent and mild vasodilator of coronary and peripheral vessels respectively 30 which reduces peripheral resistance and afterload though not as potent as the dihydropyridine DHP calcium channel blockers This results in minimal reflexive sympathetic changes citation needed Diltiazem has negative inotropic chronotropic and dromotropic effects This means diltiazem causes a decrease in heart muscle contractility how strong the beat is lowering of heart rate due to slowing of the sinoatrial node and a slowing of conduction through the atrioventricular node increasing the time needed for each beat Each of these effects results in reduced oxygen consumption by the heart reducing angina typically unstable angina symptoms These effects also reduce blood pressure by causing less blood to be pumped out Research EditDiltiazem is prescribed off label by doctors in the US for prophylaxis of cluster headaches Some research on diltiazem and other calcium channel antagonists in the treatment and prophylaxis of migraine is ongoing 15 31 32 33 34 35 36 needs update Recent research when has shown diltiazem may reduce cocaine cravings in drug addicted rats 37 This is believed to be due to the effects of calcium blockers on dopaminergic and glutamatergic signaling in the brain 38 Diltiazem also enhances the analgesic effect of morphine in animal tests without increasing respiratory depression 39 and reduces the development of tolerance 40 Diltiazem is also being used in the treatment of anal fissures It can be taken orally or applied topically with increased effectiveness 41 When applied topically it is made into a cream form using either vaseline or Phlojel Phlojel absorbs the diltiazem into the problem area better than the vaseline base It has good short term success rates 42 43 References Edit a b Diltiazem Use During Pregnancy Drugs com 4 May 2020 Retrieved 5 May 2020 Dilcardia SR 120 mg Prolonged release hard capsules Summary of Product Characteristics SmPC emc 22 March 2018 Archived from the original on 28 August 2021 Retrieved 13 April 2020 Angitil SR XL Capsules Summary of Product Characteristics SmPC emc 7 May 2019 Retrieved 13 April 2020 Cardizem diltiazem hydrochloride tablet coated DailyMed 2 June 2020 Retrieved 23 October 2022 Cardizem CD diltiazem hydrochloride capsule coated extended release DailyMed 30 April 2020 Retrieved 23 October 2022 Cardizem LA diltiazem hydrochloride tablet extended release DailyMed 2 May 2019 Retrieved 23 October 2022 Active substance s diltiazem PDF European Medicines Agency 11 January 2018 a b c d e f g h i j k Diltiazem Hydrochloride Monograph for Professionals Drugs com AHFS Retrieved 28 December 2018 Cardiovascular Pharmacotherapeutics Cardiotext Publishing 2011 pp 251 52 ISBN 978 1935395621 Retrieved 28 December 2018 2010 Nurse s Drug Handbook Jones amp Bartlett Learning 2010 p 320 ISBN 978 0763779009 Milne GW 2005 Gardner s Commercially Important Chemicals Synonyms Trade Names and Properties John Wiley amp Sons p 223 ISBN 978 0471736615 Retrieved 28 December 2018 The Top 300 of 2020 ClinCalc Retrieved 7 October 2022 Diltiazem Drug Usage Statistics ClinCalc Retrieved 7 October 2022 Diltiazem hydrochloride diltiazem hydrochloride extended release tablets tablet extended release DailyMed 1 April 2019 Retrieved 13 April 2020 a b Grossman E Messerli FH 2004 Calcium antagonists Progress in Cardiovascular Diseases 47 1 34 57 doi 10 1016 j pcad 2004 04 006 PMID 15517514 Claas SA Glasser SP May 2005 Long acting diltiazem HCl for the chronotherapeutic treatment of hypertension and chronic stable angina pectoris Expert Opinion on Pharmacotherapy 6 5 765 776 doi 10 1517 14656566 6 5 765 PMID 15934903 S2CID 39272285 Gabrielli A Gallagher TJ Caruso LJ Bennett NT Layon AJ October 2001 Diltiazem to treat sinus tachycardia in critically ill patients a four year experience Critical Care Medicine 29 10 1874 1879 doi 10 1097 00003246 200110000 00004 PMID 11588443 S2CID 25104288 Wattanasuwan N Khan IA Mehta NJ Arora P Singh N Vasavada BC Sacchi TJ February 2001 Acute ventricular rate control in atrial fibrillation IV combination of diltiazem and digoxin vs IV diltiazem alone Chest 119 2 502 506 doi 10 1378 chest 119 2 502 PMID 11171729 Basile J November 2004 The role of existing and newer calcium channel blockers in the treatment of hypertension Journal of Clinical Hypertension 6 11 621 629 quiz 630 631 doi 10 1111 j 1524 6175 2004 03683 x PMC 8109670 PMID 15538095 S2CID 23440538 Griffin N Acheson AG Jonas M Scholefield JH October 2002 The role of topical diltiazem in the treatment of chronic anal fissures that have failed glyceryl trinitrate therapy Colorectal Disease 4 6 430 435 doi 10 1046 j 1463 1318 2002 00376 x PMID 12790914 S2CID 32959944 Ramoska EA Spiller HA Winter M Borys D February 1993 A one year evaluation of calcium channel blocker overdoses toxicity and treatment Annals of Emergency Medicine 22 2 196 200 doi 10 1016 S0196 0644 05 80202 1 PMID 8427431 Talreja O Cassagnol M 2019 Diltiazem StatPearls Treasure Island FL StatPearls Publishing PMID 30422532 Solhjoo M Ho CH Chauhan E 2019 article 24529 Drug Induced Lupus Erythematosus Treasure Island FL StatPearls Publishing PMID 28722919 Retrieved 20 November 2019 Ohno Y Hisaka A Suzuki H 2007 General framework for the quantitative prediction of CYP3A4 mediated oral drug interactions based on the AUC increase by coadministration of standard drugs Clinical Pharmacokinetics 46 8 681 696 doi 10 2165 00003088 200746080 00005 PMID 17655375 S2CID 41343222 Edoute Y Nagachandran P Svirski B Ben Ami H April 2000 Cardiovascular adverse drug reaction associated with combined beta adrenergic and calcium entry blocking agents Journal of Cardiovascular Pharmacology 35 4 556 559 doi 10 1097 00005344 200004000 00007 PMID 10774785 Narimatsu A Taira N August 1976 Effects of atrio ventricular conduction of calcium antagonistic coronary vasodilators local anaesthetics and quinidine injected into the posterior and the anterior septal artery of the atrio ventricular node preparation of the dog Naunyn Schmiedeberg s Archives of Pharmacology 294 2 169 177 doi 10 1007 bf00507850 PMID 1012337 S2CID 21986119 Drug interactions Interactions between fentanyl and drugs that inhibit CYP3A4 Archived from the original on 3 December 2017 Retrieved 26 June 2019 Matsumae H Akatsuka H Shibatani T 2010 Diltiazem Synthesis Encyclopedia of Industrial Biotechnology doi 10 1002 9780470054581 eib603 ISBN 978 0471799306 O Connor SE Grosset A Janiak P 1999 The pharmacological basis and pathophysiological significance of the heart rate lowering property of diltiazem Fundamental amp Clinical Pharmacology 13 2 145 153 doi 10 1111 j 1472 8206 1999 tb00333 x PMID 10226758 S2CID 20440286 Gordon SG Kittleson MD 2008 Drugs used in the management of heart disease and cardiac arrhythmias Small Animal Clinical Pharmacology Elsevier pp 380 457 doi 10 1016 b978 070202858 8 50019 1 ISBN 978 0 7020 2858 8 Montastruc JL Senard JM April 1992 Calcium channel blockers and prevention of migraine Calcium channel blockers and prevention of migraine Pathologie Biologie in French 40 4 381 388 PMID 1353873 Kim KE February 1991 Comparative clinical pharmacology of calcium channel blockers American Family Physician 43 2 583 588 PMID 1990741 Andersson KE Vinge E March 1990 Beta adrenoceptor blockers and calcium antagonists in the prophylaxis and treatment of migraine Drugs 39 3 355 373 doi 10 2165 00003495 199039030 00003 PMID 1970289 S2CID 13621196 Paterna S Martino SG Campisi D Cascio Ingurgio N Marsala BA July 1990 Evaluation of the effects of verapamil flunarizine diltiazem nimodipine and placebo in the prevention of hemicrania A double blind randomized cross over study La Clinica Terapeutica 134 2 119 125 PMID 2147612 Smith R Schwartz A May 1984 Diltiazem prophylaxis in refractory migraine The New England Journal of Medicine 310 20 1327 1328 doi 10 1056 NEJM198405173102015 PMID 6144044 Peroutka SJ November 1983 The pharmacology of calcium channel antagonists a novel class of anti migraine agents Headache 23 6 278 283 doi 10 1111 j 1526 4610 1983 hed2306278 x PMID 6358127 S2CID 40215836 Common Heart Drug May Reduce Cocaine Cravings Sciencedaily com 28 February 2008 Retrieved on 2012 10 21 Mills K Ansah TA Ali SF Mukherjee S Shockley DC July 2007 Augmented behavioral response and enhanced synaptosomal calcium transport induced by repeated cocaine administration are decreased by calcium channel blockers Life Sciences 81 7 600 608 doi 10 1016 j lfs 2007 06 028 PMC 2765982 PMID 17689567 Kishioka S Ko MC Woods JH May 2000 Diltiazem enhances the analgesic but not the respiratory depressant effects of morphine in rhesus monkeys European Journal of Pharmacology 397 1 85 92 doi 10 1016 S0014 2999 00 00248 X PMID 10844102 Verma V Mediratta PK Sharma KK July 2001 Potentiation of analgesia and reversal of tolerance to morphine by calcium channel blockers Indian Journal of Experimental Biology 39 7 636 642 PMID 12019755 Jonas M Neal KR Abercrombie JF Scholefield JH August 2001 A randomized trial of oral vs topical diltiazem for chronic anal fissures Diseases of the Colon and Rectum 44 8 1074 1078 doi 10 1007 BF02234624 PMID 11535842 S2CID 40406260 Nash GF Kapoor K Saeb Parsy K Kunanadam T Dawson PM November 2006 The long term results of diltiazem treatment for anal fissure International Journal of Clinical Practice 60 11 1411 1413 doi 10 1111 j 1742 1241 2006 00895 x PMID 16911570 S2CID 23510129 Sajid MS Rimple J Cheek E Baig MK January 2008 The efficacy of diltiazem and glyceryltrinitrate for the medical management of chronic anal fissure a meta analysis International Journal of Colorectal Disease 23 1 1 6 doi 10 1007 s00384 007 0384 x PMID 17846781 S2CID 13015745 External links Edit Diltiazem Drug Information Portal U S National Library of Medicine Portal Medicine Retrieved from https en wikipedia org w index php title Diltiazem amp oldid 1170061904, wikipedia, wiki, book, books, library,

article

, read, download, free, free download, mp3, video, mp4, 3gp, jpg, jpeg, gif, png, picture, music, song, movie, book, game, games.