Dynacrine
Dynacrine - General Information
A potent antagonist of calcium channels that is highly selective for vascular smooth muscle. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure. [PubChem]
Pharmacology of Dynacrine
Dynacrine, the most potent calcium-channel blocking agent of the dihydropyridine class, is similar to nifedipine, amlodipine, and felodipine. It binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and smooth muscle. The effects observed in mechanistic experiments in vitro and studied in intact animals and man are compatible with this mechanism of action and are typical of the class.
Dynacrine for patients
Description
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For those patients who have high blood pressure, and is sometime used to treat angina
(chest pains).
General Information
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This information is for educational purposes only. Not every known side effect, adverse
effect, or drug interaction is in this database. If you have questions about your medicines,
talk to your healthcare provider.
Proper use of this medicine
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Take this medicine exactly as directed. This medicine is normally taken once daily. It is
taken orally and may be taken with or without food. The extended-release tablet and capsule
should be swallowed whole. Do not chew, divide, or crush the extended-release tablet or
capsule.
Missed Dose
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Take your next dose as soon as you remember. If it is time for your next dose, skip the
missed dose and go back to your regular schedule. Do not double doses.
Storage
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Keep this medication in the container it came in, tightly closed, and out of reach of
children. Store it at room temperature and away from excess heat and moisture. Throw away
any medication that is outdated or no longer needed.
Possible Side Effects
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If you experience other bothersome side effects, contact your health care provider.
Some common side effects reported with this medicine include:
nausea
dizziness
headache
swelling
Warnings/Precautions
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Do not stop suddenly stop this medicine without talking to your doctor.
This medicine can cause dizziness. Use caution when operating a motor vehicle.
Overdose
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Seek medical attention immediately. For non emergencies, contact your local or regional
poison control center
Drug Interactions
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Tell your doctor and pharmacist about all other medicines that you are taking, including
non-prescription medicines, nutritional supplements, or herbal products.
Pregnancy/Nursing
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If you suspect that you may be pregnant, talk to your doctor. There are no clear answers,
but animal studies suggest caution during pregnancy, and use should only be when risks are
outweighed by possible benefits. For nursing mothers, it is not known if amlodipine is
excreted in breast milk, so caution is recommended.
More Information
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For more information about this medicine, talk to your healthcare provider.
Dynacrine Interactions
Nitroglycerin: DynaCirc® (isradipine) has been safely coadministered with nitroglycerin.
Hydrochlorothiazide: A study in normal healthy volunteers has shown that concomitant administration of DynaCirc® (isradipine) and hydrochlorothiazide does not result in altered pharmacoktnetics of either drug. In a study in hypertensive patients, addition of isradipine to existing hydrochlorothiazide therapy did not result in any unexpected adverse effects, and isradipine had an additional antihypertensive effect.
Propranolol: In a single dose study in normal volunteers, coadministration of propranolol had a small effect on the rate but no effect on the extent of isradipine bioavailability. Significant increases In AUC (27%) and Cmax (58%) and decreases in tmax (23%) of propranolol were noted in this study. However, concomitant administration of 5 mg b.i.d. isradipine and 40 mg b.i.d. propranolol to healthy volunteers under steady-state conditions had no relevant effect on either drugís bioavailability, AUC and Cmax, differences were <20% between isradipine given singly and in combination with propranolol, and between propranolol given singly and in combination with isradipine.
Cimetidine: In a study in healthy volunteers, a one-week course of cimetidine at 400 mg b.i.d. with a single 5 mg dose of isradipine on the sixth day showed an increase in isradipine mean peak plasma concentrations (36%) and significant increase in area under the curve (50%). If isradipine therapy is initiated in a patient currently receiving cimetidine careful monitoring for adverse reactions is advised and downward dose adjustment may be required.
Rifampicin: In a study in healthy volunteers, a six-day course of rifampicin at 600 mg/day followed by a single 5 mg dose of isradipine resulted in a reduction in isradipine levels to below detectable limits. If rifampicin therapy is required, isradipine concentrations and therapeutic effects are likely to be markedly reduced or abolished as a consequence of increased metabolism and higher clearance of isradipine.
Warfarin: In a study in healthy volunteers, no clinically relevant pharmacokinetic or pharmacodynamic interaction between isradipine and racemic warfarin was seen when two single oral doses of warfarin (0.7 mg/kg body weight) were administered during 11 days of multipledose treatment with 5 mg b.i.d. isradipine. Neither racemic warfarin nor isradipine binding to plasma proteins in vitro was altered by the addition of the other drug.
Digoxin: The concomitant administration of DynaCirc® (isradipine) and digoxin in a single-dose pharmacokinetic study did not affect renal, nonrenal and total body clearance of digoxin.
Fentanyl Anesthesia: Severe hypotension has been reported during fentanyl anesthesia with concomitant use of a beta blocker and a calcium channel blocker. Even though such interactions have not been seen in clinical studies with DynaCirc® (isradipine), an increased volume of circulating fluids might be required if such an interaction were to occur.
Dynacrine Contraindications
DynaCirc® (isradipine) is contraindicated in individuals who have shown hypersensitivity to any of the ingredients in the formulation.
Additional information about Dynacrine
Dynacrine Indication: For the management of hypertension. It may be used alone or concurrently with thiazide-type diuretics.
Mechanism Of Action: Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, isradipine inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Isradipine
Synonyms: (+-)-Isradipine; (+/-)-Isradipine; Isradipino [Spanish]; Isradipinum [Latin]; Isrodipine; Isradipin
Drug Category: Calcium Channel Blockers; Vasodilator Agents; Antihypertensive Agents
Drug Type: Small Molecule; Approved
Other Brand Names containing Isradipine: Clivoten; DynaCire; DynaCire CR; DynaCirc; Dynacirc CR; Dynacrine; Esradin; Lomir; Prescal; Rebriden; Absorption: Isradipine is 90%-95% absorbed and is subject to extensive first-pass metabolism, resulting in a bioavailability of about 15%-24%.
Toxicity (Overdose): Symptoms of overdose include lethargy, sinus tachycardia, and transient hypotension. Significant lethality was observed in mice given oral doses of over 200 mg/kg and rabbits given about 50 mg/kg of isradipine. Rats tolerated doses of over 2000 mg/kg without effects on survival.
Protein Binding: 95%
Biotransformation: Hepatic. Completely metabolized prior to excretion and no unchanged drug is detected in the urine.
Half Life: 8 hours
Dosage Forms of Dynacrine: Capsule Oral
Chemical IUPAC Name: O5-methyl O3-propan-2-yl 4-(2,1,3-benzoxadiazol-7-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
Chemical Formula: C19H21N3O5
Isradipine on Wikipedia: https://en.wikipedia.org/wiki/Isradipine
Organisms Affected: Humans and other mammals
