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- Pharmacology For Isosorbide-5-Mononitrate + Aspirin (Low Dose)
Isosorbide-5-Mononitrate + Aspirin (Low Dose) Pharmacology
Isosorbide-5-Mononitrate + Aspirin (Low Dose)About Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AMechanism of Action of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/APharmacokinets of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AOnset of Action for Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/ADuration of Action for Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AHalf Life of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/ASide Effects of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AContra-indications of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/ASpecial Precautions while taking Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/APregnancy Related InformationN/AOld Age Related InformationN/ABreast Feeding Related InformationN/AChildren Related InformationN/AIndications for Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AInteractions for Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/ATypical Dosage for Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/ASchedule of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AStorage Requirements for Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AEffects of Missed Dosage of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/AEffects of Overdose of Isosorbide-5-Mononitrate + Aspirin (Low Dose)N/A
Isosorbide-5-MononitrateAbout Isosorbide-5-MononitrateAlkyl nitrate derivative, a direct vasodilator, Antianginal.Mechanism of Action of Isosorbide-5-MononitrateIt is a direct smooth muscle relaxant, which have a prominent action vascular smooth muscles preferentially veins than arteries. It is enzymatically denitrated in the smooth muscle cells to release the reactive free radical nitric oxide which activates cytosolic guanylyl cyclase thus increases cyclic GMP levels which causes dephosphorylation of myosin light chain kinase(MLCK) through a cyclic GMP dependent protein kinase. Reduced availability of phosphorylated (active) MLCK interferes with activation of myosin and myosin fails to interact with actin to cause contraction and consequently relaxation occurs. Elevated levels of cyclic GMP also reduce calcium entry which also contributing to relaxation. It dilates veins more than arteries because veins have greater amount of enzyme that generate nitric oxide from nitrates. It also preferentially dilates epicardial arteries than autoregulatory arteries duo to defferential distribution of nitrate metabolizing enzymes in these vessels.
It causes preload reduction, slight decrease in after load, and preferential relaxation of larger conducting coronary arteries and is used as an effective drug in the management of both angina and congestive heart failure.
Pharmacokinets of Isosorbide-5-MononitrateAbsorption: Well absorbed orally, bioavailability is about 100%.Onset of Action for Isosorbide-5-Mononitrate30 to 60 minutesDuration of Action for Isosorbide-5-MononitrateN/AHalf Life of Isosorbide-5-Mononitrate4 to 6 hoursSide Effects of Isosorbide-5-Mononitrate1. Headache
7. Orthostatic hypotension
9. Sub lingual burning
Contra-indications of Isosorbide-5-Mononitrate1. Myocardial infarction
2. Hypersensitivity to nitrates
3. Severe hypotension
5. Along with phosphodiesterase inhibitors
Special Precautions while taking Isosorbide-5-Mononitrate1. Gradually withdraw the drug with caution start therapy with lower doses
3. Blood volume depletetion
4. Cerebral haemorrhage
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationContraindicatedIndications for Isosorbide-5-Mononitrate1. Prophylaxis of angina pectoris
2. Adjunctive treatment of heart failure
3. Post myocardial infarction therapy
Interactions for Isosorbide-5-MononitrateAlcohol: Severe hypotension and cardiovascular collapse.
Aspirin: Increase serum concentrations of nitrates and their actions.
Antihypertensives, TCAs, Phenothiazine, Calcium channel blockers: Marked symptomatic orthostatic hypotension.
Lab Tests: May interfere with the Zlatkis-Zak colour reaction causing a false report of decreased serum cholesterol.Typical Dosage for Isosorbide-5-Mononitrate10 to 20mg two times daily with 7 hours apart; and first dose in morning.
Sustained release forms: 30 to 60mg once daily; Increased to 120mg once daily if required.
Schedule of Isosorbide-5-MononitrateHStorage Requirements for Isosorbide-5-MononitrateStore at a temperature below 25 degree C. Protects from moisture.Effects of Missed Dosage of Isosorbide-5-MononitrateN/AEffects of Overdose of Isosorbide-5-MononitrateTreatment is supportive and symptomatic. Remove drug from the body by gastric lavage and administer activated charcoal to reduce absorption. Monitor blood gas measurements and methemoglobin levels. Supportive measures include respiratory support and oxygen administration. Recumbent positioning and passive movements of the extremities aid venous return. Maintain adequate body temperature and administer I.V. fluids. Administer adrenergic agonist like phenylephrine if required. For Methaemoglobinaemia; methylene blue may be given.
Aspirin (Low Dose)About Aspirin (Low Dose)Salicylate, Anti platelet.Mechanism of Action of Aspirin (Low Dose)The drug exerts it`s antithrombotic action by interfering with platelet aggregation. It irreversibly inactivating and inhibiting the enzymes cyclooxygenase and thromboxane-synthetase. At lower doses it selectively suppresses the release of thromboxane-A2 till fresh platelets are formed. It also inhibits the release of ADP from platelets and their sticking to each other.Pharmacokinets of Aspirin (Low Dose)Absorption: Well absorbed orally, Distribution: Widely distributed in the body in a protein bound form, Metabolism: Metabolized in the liver in to metabolites. Excretion: Excreted through urine as salicylates and it`s metabolites.Onset of Action for Aspirin (Low Dose)N/ADuration of Action for Aspirin (Low Dose)5 to 7daysHalf Life of Aspirin (Low Dose)15 to 20minutesSide Effects of Aspirin (Low Dose)1.Prolonged bleeding time
Contra-indications of Aspirin (Low Dose)1.Hypersensitivity to the drug
3.Severe renal impairment
4.Severe hepatic impairment
Special Precautions while taking Aspirin (Low Dose)
4.In gastrointestinal lesions
5.Vitamin K deficiency
6.Thrombotic thrombocytopenic purpura
Pregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationContraindicatedChildren Related InformationContraindicatedIndications for Aspirin (Low Dose)Prophylaxis treatment of increased risks of blood clottingInteractions for Aspirin (Low Dose)Drugs Affecting Aspirin:
Activated charcoal: Decreases absorption of aspirin.
Antacids Urinary alkalizers and Cortiosteroids: Decrease efficacy of aspirin.
Drugs affected by aspirin:
Alcohol: Risk of G.I. ulceration increases; may also prolong bleeding time.
ACE inhibitors: Antihypertensive action decreased.
Oral Anticoagulants : May potentiate effect.
Methotrexate: Effect potentiated.
Tetracycline: Efficacy decreased.
Tricyclic Antidepressants - Effect potentiated.
Nitroglycerin: May result in unexpected hypotension.
Beta-adrenergic Blockers - Antihypertensive effect blunted.
NSAIDs: May decrease serum concentration.
Sulfonylureas and Exogenous Insulin: In high doses may potentiate these drugs.
Valproic Acid: Potentiates effect.
Spironolactone: May inhibit diuretic effect.
Probenecid & Sulfinpyrazone : Antagonise uricosuric effect (In doses > 3gm/day - uricosuric effect)
Thyroid Function Tests: Increase in PBI
Serum Uric Acid Levels: Increased by levels less than 10 mg/dl and decreased by levels> 10 mg/dl.
Urine Glucose: False negative by glucose oxidase method. False positive results by reduction method.
Urinary Ketones: Produce reddish colour.Typical Dosage for Aspirin (Low Dose)0ral: 50mg to 160mg/daySchedule of Aspirin (Low Dose)HStorage Requirements for Aspirin (Low Dose)Store at room temperature and protects from moisture.Effects of Missed Dosage of Aspirin (Low Dose)Take the missed dose as soon as noticed and if it is the time for next dose then skip the missed dose. Continue the regular schedule. Do not double the dose.Effects of Overdose of Aspirin (Low Dose)Empty stomach by induced emesis and gastric lavage. Reduce absorption by administration of activated charcoal. Give symptomatic and supportive treatment. Monitor and assist respiratory function, fluid and electrolyte balance, and other vital parameters. Administer sodium bicarbonate and enhance alkaline diuresis. Haemodialysis is effective in severe poisoning.
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