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- Pharmacology For Isosorbide Dinitrate + Hydralazine
Isosorbide Dinitrate + Hydralazine Pharmacology
Isosorbide Dinitrate + Hydralazine
About Isosorbide Dinitrate + HydralazineN/AMechanism of Action of Isosorbide Dinitrate + HydralazineN/APharmacokinets of Isosorbide Dinitrate + HydralazineN/AOnset of Action for Isosorbide Dinitrate + HydralazineN/ADuration of Action for Isosorbide Dinitrate + HydralazineN/AHalf Life of Isosorbide Dinitrate + HydralazineN/ASide Effects of Isosorbide Dinitrate + HydralazineN/AContra-indications of Isosorbide Dinitrate + HydralazineN/ASpecial Precautions while taking Isosorbide Dinitrate + HydralazineN/APregnancy Related InformationContraindicatedOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationContraindicatedIndications for Isosorbide Dinitrate + HydralazineTreatment of heart failure as an adjunct to standard therapy in self-identified black patients to improve survival,to prolong time to hospitalization for heart failure,and to improve patient-reported functional status.Interactions for Isosorbide Dinitrate + HydralazineN/ATypical Dosage for Isosorbide Dinitrate + HydralazineN/ASchedule of Isosorbide Dinitrate + HydralazineN/AStorage Requirements for Isosorbide Dinitrate + HydralazineN/AEffects of Missed Dosage of Isosorbide Dinitrate + HydralazineN/AEffects of Overdose of Isosorbide Dinitrate + HydralazineN/AIsosorbide Dinitrate
About Isosorbide DinitrateAlkyl nitrate derivative, a direct vasodilator, Antianginal.Mechanism of Action of Isosorbide DinitrateIt 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 DinitrateAbsorption: Well absorbed orally, But bioavailability is reduced due to first pass metabolism.
Distribution: Widely distributed in the body.
Metabolism: Metabolized in liver to active metabolites.
Excretion: Excreted mainly through urine.
Onset of Action for Isosorbide DinitrateSub lingual: 3 minutes
Oral: 30 minutes
Duration of Action for Isosorbide DinitrateSub lingual: Half to Two hours
Oral: 5 to 6 hours
Half Life of Isosorbide DinitrateSub lingual: 2 hours
Oral: 5 to 6 hours
Side Effects of Isosorbide Dinitrate1. Headache
2. Weakness
3. Dizziness
4. Methaemoglobinaemia
5. Flushing
6. Palpitation
7. Orthostatic hypotension
8. Sweating
9. Sub lingual burning
10. Rashes
Contra-indications of Isosorbide Dinitrate1. Myocardial infarction
2. Hypersensitivity to nitrates
3. Severe hypotension
4. Shock
5. Along with phosphodiesterase inhibitors
Special Precautions while taking Isosorbide Dinitrate1. Gradually withdraw the drug with caution
2. Hypotension
3. Blood volume depletetion
4. Cerebral haemorrhage
5. Glaucoma
6. Sidenafil causes dangerous potentiation of action hypotension myocardial infarction and death
Pregnancy Related InformationUse with cautionOld Age Related InformationUse with cautionBreast Feeding Related InformationUse with cautionChildren Related InformationContraindicatedIndications for Isosorbide Dinitrate1. Classical angina
2. Variant angina
3. Adjunctive treatment of heart failure
4. Esophageal spasm without gastroesophagial reflux.
Interactions for Isosorbide DinitrateAlcohol: 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 DinitrateDosage:
Sublingual form: 2.5 to 10mg. Repeated every 2 to 3 hours during acute phase or every 4 to 6 hours for prophylaxis.
Chewable form: Starts with 5mg test dose and increased up to 10mg as required for acute attack or every 2 to 3 hours for prophylaxis.
Oral form: 10 to 20mg three to four times daily for prophylaxis
Extended release form: 20 to 40mg 2 - 3 times daily.
Schedule of Isosorbide DinitrateHStorage Requirements for Isosorbide DinitrateStore in a cool place away from flame and heat and protects from moisture in a tightly closed container.Effects of Missed Dosage of Isosorbide DinitrateTake the missed dose as soon as remember and If it is the time for next dose then skip the missed dose and take the regular dose.Effects of Overdose of Isosorbide DinitrateTreatment 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.Hydralazine
About HydralazineA direct-acting smooth muscle relaxant, Pyridazine derivative, Antihypertensive(Vasodilator).Mechanism of Action of HydralazineHydralazine exerts its pharmacological actions by direct vasodilator action on arteriolar smooth muscles with little actions on venous capacitance vessels. It produces after load reduction by dilating resistance vessels which leads to decreasing aortic impedence.So that more blood is pumped even in weaker ventricular contractions. It decreases total peripheral resistance and there is greater decrease in diastolic pressure than systolic pressure. There is a decrease in intracellular Ca2+concentration but there is no reduction in renal blood flow.Pharmacokinets of HydralazineAbsorption: It is well absorbed orally, but bioavailability is low in fast acetylators.Distribution: Widely distributed in a highly plasma protein bound form.Metabolism: It is metabolized in liver,plasma and gastrointestinal mucosa. Excretion: Excreted mainly through urine and the rest of dose is excreted through bile and faeces.
Onset of Action for Hydralazine10 to 30 minutesDuration of Action for HydralazineUp to 6 hoursHalf Life of Hydralazine1 hourSide Effects of Hydralazine1. Tachycardia
2. Tachyphylaxis
3. Edema
4. Palpitation
5. Dizziness
6. Dryness of mouth
7. Nasal congestion
8. Headache
9. Palpitation
10. Weakness
11. Orthostatic hypotension
12. Angina
13. Anxiety
14. Sleep disturbances
15. Reversible lupus erythmatosis
16. Paraeshesia
17. Tremor
18. Muscle cramps
Contra-indications of Hydralazine1. Hypersensitivity to the drug,
2. Ischaemic heart disease
3. Coronary artery diseases
4. Valvular stenosis
5. Pericarditis
6. Aortic aneurism
Special Precautions while taking Hydralazine1. Renal impairment
2. Hepatic impairment
3. Cardiovascular disorders
4. Cerebro vascular disorders
5. Use with caution along with other antihypertensive drugs
6. Slowly withdraw the drug with caution
Pregnancy Related InformationUse with cautionOld Age Related InformationContraindicatedBreast Feeding Related InformationContraindicatedChildren Related InformationUse with cautionIndications for Hydralazine1. Hypertension
2. Congestive heart failure
3. Pregnancy associated hypertensive crisis
4. Hypertension associated with renal involvement
Interactions for HydralazineMAOIs, Thiazide diuretics & TCAs: Antihypertensive effect of hydralazine enhanced.
Sympathomimetics: Use these agents with great caution since hydralazine alone may cause tachycardia and angina.
Propranolol, Metoprolol: Oral bioavailability of these agents may be increased. Also they counteract reflex tachycardia.
Parenteral antihypertensive drugs: (e.g. Diazoxide): Profound hypotensive episodes may occur.
Alcohol: Hydralazine potentiates effect of alcohol.Typical Dosage for HydralazineHypertension:
Oral: Starts with 10mg 6th hourly. Increase the dosage up to 25mg 12th hourly to 6th hourly or 50mg 12th hourly to 6th hourly depending up on the patient`s response.
Maximum daily dose: 200mg
Maximum dose in fast acetylators: 300 to 400mg/day
I.V.: 10 to 20mg. Repeat if required by the patient
Children: Starts with 0.75mg/day. Increased up to 7.5mg/kg/day based on patient`s response.
Heart failure: Starts with 50 to 75mg. Increase the dosage up to 200 to 600mg/day in 2 to 4 divided doses based on patient`s response.
Maximum dose: 3gm/day
Pregnancy associated hypertensive crisis: Starts with 5mg I.V. Increases to 10mg at every half an hour until desired response is obtained.
Schedule of HydralazineHStorage Requirements for HydralazineStore at controlled room temperature at a temperature range of 15 to 30 degree C in a light resistant tightly closed container.Effects of Missed Dosage of HydralazineTake 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 HydralazineTreatment is supportive and symptomatic. After ingestion empty the stomach by induced emesis and gastric lavage. Administer activated charcoal to reduce absorption. Home Delivery for Isosorbide Dinitrate + Hydralazine in Your City
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Isosorbide Dinitrate + Hydralazine is a generic medicine name and there are several brands available for it. Some of the brands for isosorbide dinitrate + hydralazine might be better known than isosorbide dinitrate + hydralazine itself. If the pharmacy that's willing to deliver medicines to your home doesn't have isosorbide dinitrate + hydralazine in stock, you can ask for one of the branded alternatives for isosorbide dinitrate + hydralazine.
