Cimetidine (HCl)

Cimetidine (HCl) is a histamine H2 receptor blocking agent. It conatins a substituted imidazole ring. Cimetidine approved for clinical use in 1977 by the Food and Drug Aministration and after five years of clinical experience of cimetidine in 25 million patients, cimetidine is considered the prototype drug for ulcer therapy.


Adult Dose
Dose: 400 mg
Single Dose: 400 (400)
Frequency: 12 hourly
Route: PO
Instructions: For 6 weeks.
Neonatal
Dose: 20 mg/kg
Single Dose: 20 (20)
Frequency: As recommended.
Route: oral
Instructions: in divided doses
Paedriatic
Dose: 25 to 30 mg/kg
Single Dose: 28 (27.5)
Frequency: As recommended.
Route: Oral
Instructions: in divided doses
Characteristics
Cimetidine is the derivative of Cimetidine (HCl). It is of Synthetic origin and belongs to Imidazole Guanidine. It belongs to H2-antagonist pharmacological group on the basis of mechanism of action and also classified in Antineoplastic Agent, Plant Derivative pharmacological group.The Molecular Weight of Cimetidine (HCl) is 288.80. Its pKa is 7.1.
Contraindications
Cimetidine (HCl) is contraindicated in conditions like Hypersensitivity.
Effects
The severe or irreversible adverse effects of Cimetidine (HCl), which give rise to further complications include Tachycardia, Fever, Thrombocytopenia, Aplastic anemia, Aplastic anemia, Stevens johnson syndrome, Impotence, Jaundice, Jaundice, Stevens johnson syndrome, Granulocytopenia, Agranulocytosis, Interstitial nephritis, Acute pancreatitis, Reversible confusion state, Acute pancreatitis, Sinus bradycardia, Gynacomastia, Aplastic anemia, reversible on stoping treatment.Cimetidine (HCl) produces potentially life-threatening effects which include Cardiac arrhythmia, Heart block. which are responsible for the discontinuation of Cimetidine (HCl) therapy.The symptomatic adverse reactions produced by Cimetidine (HCl) are more or less tolerable and if they become severe, they can be treated symptomatically, these include Dizziness, Tiredness, Headache, Alopecia, Diarrhea, Fever, Myalgia, Rashes, Confusion, Hallucination, Depression, Arthralgia, Agitation, Confusion, Alopecia, dizziness, plasma creatinine level increase, Sr parathyroid hormone increase, HDL chlosterol level increase.
Indications
Cimetidine (HCl) is primarily indicated in conditions like Acid-related dyspepsia, Aspiration prophylaxis, Benign gastric and duodenal ulceration, Degradation of pancreatic enzyme suppliments, Duodenal ulcer, Dyspepsia, Gastric acid reduction (surgical procedures), Gastric ulceration, Mendelsons syndrome prophylaxis, NSAID associated ulceration, NSAID-induced ulcer prophylaxis, Peptic ulcer, Prohylaxis of stress ulceration, Prophylaxis of acid aspiration in obstetric patients, Reflux oesophagitis, Risk of acid aspiration in obstetric patients, Short-bowel syndrome, Stress ulcers prevention, Surgical procedures, To reduce degradation of pancreatic enzyme supplements, Zollinger-ellison syndrome, and can also be given in adjunctive therapy as an alternative drug of choice in Benign gastric ulcer, Esophagitis, Gastritis, GI bleeding, Heart burn, Pancreatic insufficiency.
Interactions
Cimetidine (HCl) is known to interact with other drugs, the details of drug interactions is as follows:DrugDetailsSeverityOnsetManagementAcrosoxacinAdinazolamAlbendazoleAlprazolamAluminium Hydroxide and OxideAminophyllineAmisulprideAmitriptyline (HCl)Amlodipine (Besylate)Cimetidine may decrease the metabolism of Amlodipine. ModerateMonitor for increased effects of Amlodipine if Cimetidine is initiated/dose increased, and decreased effects if Cimetidine is discontinued/dose decreased. AnastrazoleAtorvastatinCimetidine may decrease the metabolism of Atorvastatin. ModeratePatients who require concomitant thaerapy should be monitored for altered antihypertensive response if Cimetidine is introduced or discontinued, or when its dosage is modified.BamifyllineBisoprolol (Fumarate)BromazepamBupropion (HCl)CaffeineCarbamazepineCimetidine inhibit the metabolism of carbamazepine.CarmustineChloramphenicolChlordiazepoxide (HCl)Chlormethiazole (Edisylate)ChloroquineChlorpromazine (HCl)Cimetidine reduces the therapeutic effects of chlorpromazine.MinorReduce the dose of chlorpromazine if necessaryChlorpropamideCimetidine inhibit the hepatic metabolism of chlorpropamide or increase its absorption by altering gastric pH results in increased plasma concentration may lead to enhanced hypoglycemic effect.ModerateClosely monitor blood sugar regularly. Reduce the dose of chlorpropamide if necessary.CilostazoleCisaprideCimetidine increases the plasma concentration of cisapride by inhibiting its metabolic clearence.Increased level of cisapide results in prolongation of QT interval on ECG, ventricular arrythmia, cardiac arrest and sudden death.MajorCoadministration should be avoided. Famotidine, nizatidine, ranitidine considered as safer alternatives of cimetidine.Citalopram (HBr)ClarithromycinClobazamClomipramine (HCl)ClopidogrelClorazepate (K)ClozapineCyclosporin ACimetidine competitively inhibits creatinine clearance for renal tubular secretion,increases serum creatinine and may antagonize cyclosporine-induced inhibition of interleukin-2 production in patients treated with cyclosporine.MinorRanitidine may be preferable to cimetidine in patients using cyclosporine.DapsoneDesmopressin (Acetate)DiazepamCimetidine reduce metabolism and increase plasma concentration of diazepam through CYP450 inhibitionthus enhance sedation and it delays clearance of Diazepam.MinorPatient response and tolerance should be monitor and diazepam dose is adjusted.Diltiazem (HCl)Doxepin (HCl)Cimetidine inhibit CYP450 thus inhibit metabolism of doxepin increases its serum concentration to toxic levelsl.ModerateMonitor patient response and tolerance.Dry mouth,blurred vission,constipation,altered heart beat,dizziness and urinary retention must be reported to physician.lDoxepin.Cimetidine(HCl) impairs excretion of Doxepin.Encainide (HCl)EpirubicinErythromycinCimetidine inhibit CYP450 metabolism result in elevated plasma levels of erythromycin. ModerateNausea,vomiting,diarrhea or abdominal pain if occur consult physician.EscitalopramFelodipineFluorouracilFosinopril (Na)FosphenytoinGabapentinGallopamilGriseofulvinHydroxychloroquine (Sulphate)Hydroxyquinolone SulphateImipramine (HCl)Interferon AlphaIsosorbide (Dinitrate)Cimetidine(HCl) may decrease the metabolism of Isosorbide(Dinitrate). ModerateMonitor for increased effects of Isosorbide (Dinitrate) if Cimetidine (HCl) is initiated/dose increased, and decreased effects if Cimetidine (HCl) is discontinued/dose decreased.IsradipineKetoconazoleCimetidine decreases absorption and bioavailability of ketoconazole by increasing gastric pH thus decreases plasma ketoconazole concentration. ModerateThis combination should not be used.Fluconazole is a better replacement of ketoconazole.LabetalolLacidipineLercanidipine (HCl)LignocaineCimitidine increases lignocaine toxicity.LoratadineLornoxicamHigher plasma concentrations of lornoxicamLypressinMetformin (HCl)Cimetidine decreases the renal tubular secretion of metformin result in increased AUC upto 50% and decreases the plasma clearence upto 27% reult in increased plasma level may lead to lactic acidosis.ModerateSlowly reduce the dose of metformin. Monitor thr blood glucose level regularly. Patient should notify to physician if experience any sign of lactic acidosis.Methotrimeprazine (Maleate)Metoclopramide (HCl)Metoprolol (Tartrate)Cimetidine inhibit hepatic CYP450 and/or renal tubular secretion thus increases plasma concentration of metoprolol.ModeratePatient response and tolerance should be monitor.MetronidazoleCimetidine increases the serum concentration of metronidazole by inhibiting its hepatic metabolism.MinorMidazolamMitomycin CMizolastineConcurrent use may increase the blood level of mizolastine and could increase the risk of side effects.MoclobemideMoricizine (HCl)MorphineNicardipineNicoumaloneNifedipineCimetidine inhibit CYP450 hepatic metabolism and/or increase gastric pH result in increase plasma concnetration of nifedipine.ModerateResponse of patient and tolerance should be monitor.Adjust dose of nifedipine.Nortriptyline (HCl)Octreotide (Acetate)OxprenololConcomitant use may potentiate effect of oxprenolol.Oxtriphylline (Choline Theophyllinate)PapaveretumParacetamolParoxetineCimetidine inhibit first pass metabolism thus increases plasma concentration of paroxetine. ModerateMonitor prolong pharmacological effects of paroxetine when administered with cimetidine.Pethidine (HCl)PhenindionePhenytoin (Na)Phenytoin (Na)PimozidePindololPiroxicamPiroxicam-beta-cyclodextrinCimetidine causes moderate prolongation of the half life of piroxicam and might therefore be expected to potentiate its effectPramipexoleCimetidine in combination with pramipexole produced a 50% increase in AUC and a 40% increase in half-life.Pravastatin (Na)PrazepamPraziquantel Procainamide (HCl)Promazine (HCl)Propafenone (HCl)Propranolol (HCl)Cimetidine by inhibiting hepatic metabolism increases plasma concentration of propranolol through CYP450 inhibition. ModeratePatient response and tolerance should be monitor.Protriptyline (HCl)QuinidineQuinineRimantadineWhen a single 100 mg dose of Rimantadine was administered one hour after the initiation of cimetidine (300 mg four times a day), the apparent total rimantadine clearance of this single dose in normal healthy adults was reduced by 18%.RofecoxibCo-administration with high doses of cimetidine increased the Cmax of rofecoxib by 21%, the AUC0-120hr by 23% and the t1/2 by 15%. RoxithromycinSecnidazoleSildenafilClearance of Sildenafil is decreased due to inhibition of CYP450SpiramycinSucralfateSucralfateSulpirideTacrine (HCl)Tamsulosin HydrochlorideConcurrent use causes significant changes in both tamsulosin hydrochloride clearance (26% decrease) and exposure (44% increase in AUC). TeprenoneTerbinafine (HCl)TerfenadineCimetidine prolong QT interval leads to ventricular arrhythmias by inhibiting CYP450 thus decreasing metabolism of terfenadine.MajorReplace with safer agent like loratadine or avoid this combination.Terpin HydrateShould not use concurretly without doctors prescription.Tetanus ToxoidTheophyllineTheophyllineTiclopidine (HCl)Tocainide (HCl)TriazolamVasopressinVenlafaxine (HCl)Warfarin (Na)Cimetidine may enhance the anticoagulant effect of Warfarin. Moderate (Sequence important)If possible, use an alternative H2-antagonist. If Cimetidine must be used, monitor for increased therapeutic effects of the Warfarin when Cimetidine is initiated/dose increased, or decreased effects if Cimetidine is discontinued/dose decreased. ZalcitabineZidovudineCimetidine in competition for active tubular secretion decreases the renal clearance of zidovudine upto 56%.MinorPatients with renal impairment must avoid this combination.Zolmitriptan These interactions are sometimes beneficial and sometimes may pose threats to life. Always consult your physician for the change of dose regimen or an alternative drug of choice that may strictly be required.
Interfrence
Interfere with Gastric Juice Haemoccult Testing treatment ingestionfaecal test donot seem to be affecrted
Risks
Drug should not be given to Pregnant Mothers, patients suffering from Kidney dysfunction, and Neonates.If prescribing authority justifies the benefits of the drug against the possible damages he/she should reevaluate them and consult the reference material and previous studies.
Storage
Inj Store at room temperature. Do not Freeze. Protect from Sunlight. Tab, Susp Store in a well closed container, at room temperature. Protect from Sunlight.
Warnings
Cimetidine should be used with caution in patients with impaired kidney or liver function. Intravenous injection of cimetidine should be given slowly and intravenous infusion is recommended in patients with cardiovascular impairment. Cimetidine can mask the symptoms and allow trasient healing of gastric cancer, the potential delay in diagnosis should particularly be borne in mind in patients of middle age and over with new or recently changed dyspeptic symptoms. In patient on drug treatment or with illness that could cause falls in the blood cell count, the possibility that H2-Receptor antagonism could potentiate this effect should be borne in mind.
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