Lispine

Lispine Uses, Dosage, Side Effects, Food Interaction and all others data.

Lispine’s Class 1a activity is similar to that of quinidine in that it targets sodium channels to inhibit conduction. Lispine depresses the increase in sodium permeability of the cardiac Myocyte during Phase 0 of the cardiac action potential, in turn decreasing the inward sodium current. This results in an increased threshold for excitation and a decreased upstroke velocity.

Lispine prolongs the PR interval by lengthening both the QRS and P wave duration. This effect is particularly well suited in the treatment of ventricular tachycardia as it slows the action potential propagation through the atria to the ventricles.

Lispine does not act as a blocking agent for beta or alpha adrenergic receptors, but does have a significant negative inotropic effect on the ventricular myocardium. As a result, the use of disopyramide may reduce contractile force up to 42% at low doses and up to 100% in higher doses leading to heart failure.

This provides a possible treatment for atrial and ventricular fibrillation, as it restores pacemaker control of the tissue to the SA and AV nodes.

Lispine is an anti-arrhythmic drug indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia that are life-threatening. At therapeutic plasma levels, disopyramide shortens the sinus node recovery time, lengthens the effective refractory period of the atrium, and has a minimal effect on the effective refractory period of the AV node. Little effect has been shown on AV-nodal and His-Purkinje conduction times or QRS duration. However, prolongation of conduction in accessory pathways occurs.

Trade Name Lispine
Availability Prescription only
Generic Disopyramide
Disopyramide Other Names Disopiramida, Disopyramide, Disopyramidum
Related Drugs propranolol, amiodarone, lidocaine, verapamil, Inderal, dofetilide
Type
Formula C21H29N3O
Weight Average: 339.4745
Monoisotopic: 339.231062565
Protein binding

50%-65%

Groups Approved
Therapeutic Class Membrane stabilizing agent (Sodium channel blockers)
Manufacturer
Available Country
Last Updated: September 19, 2023 at 7:00 am
Lispine
Lispine

Uses

Lispine is used for the ventricular arrhythmias, especially after myocardial infarction, supraventricular arrhythmias.

Lispine is also used to associated treatment for these conditions: Arrhythmia of ventricular origin

How Lispine works

Lispine is a Type 1A antiarrhythmic drug (ie, similar to procainamide and quinidine). It inhibits the fast sodium channels. In animal studies Lispine decreases the rate of diastolic depolarization (phase 4) in cells with augmented automaticity, decreases the upstroke velocity (phase 0) and increases the action potential duration of normal cardiac cells, decreases the disparity in refractoriness between infarcted and adjacent normally perfused myocardium, and has no effect on alpha- or beta-adrenergic receptors.

Dosage

Lispine dosage

The recommended dose of Lispine is 400 mg /day in 4 divided doses (100 mg capsule 6 hourly).

Patients with renal insufficiency should take 100 mg capsule according to the schedule given below:

Creatinine clearance (ml/min) >15: Approximate dosing q 8 hrq 12 hrq 24 hr

Patients in whom rapid control of ventricular arrhythmia is essential, an initial loading dose of 300 mg Lispine is recommended, followed by the appropriate maintenance dosage.

Side Effects

Usually Lispine is well tolerated but occasionally in some cases dry mouth/ nose/ eye, nausea, vomiting, diarrhea, bloating, blurred vision, urinary problems, headache, skin rash, dizziness, nervousness & impotence (1-3%) may occur.

Toxicity

LD50=580 mg/kg in rats

Precaution

Lispine should not be administered to patients with cardiomyopathy and associated congestive heart failure unless the patient is digitalized and adequately compensated. Lispine should be used with caution in the presence of digitalis intoxication.

Food Interaction

  • Avoid alcohol.
  • Take with or without food. The absorption is unaffected by food.

[Moderate] MONITOR: Grapefruit juice may increase the plasma concentrations of orally administered drugs that are substrates of the CYP450 3A4 isoenzyme.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

Because grapefruit juice inhibits primarily intestinal rather than hepatic CYP450 3A4, the magnitude of interaction is greatest for those drugs that undergo significant presystemic metabolism by CYP450 3A4 (i.e., drugs with low oral bioavailability).

In general, the effect of grapefruit juice is concentration-, dose- and preparation-dependent, and can vary widely among brands.

Certain preparations of grapefruit juice (e.g., high dose, double strength) have sometimes demonstrated potent inhibition of CYP450 3A4, while other preparations (e.g., low dose, single strength) have typically demonstrated moderate inhibition.

Pharmacokinetic interactions involving grapefruit juice are also subject to a high degree of interpatient variability, thus the extent to which a given patient may be affected is difficult to predict.

MANAGEMENT: Patients who regularly consume grapefruit or grapefruit juice should be monitored for adverse effects and altered plasma concentrations of drugs that undergo significant presystemic metabolism by CYP450 3A4.

Grapefruit and grapefruit juice should be avoided if an interaction is suspected.

Orange juice is not expected to interact with these drugs.

Lispine Alcohol interaction

[Minor] Ethanol significantly increases the renal elimination of disopyramide, apparently by inducing diuresis (inhibition of antidiuretic hormone).

Limited data show that ethanol does not, however, significantly affect the elimination half-life or total plasma clearance of disopyramide. No special precautions appear to be necessary.

Elimination Route

Nearly complete

Half Life

6.7 hours (range 4-10 hours)

Elimination Route

In healthy men, about 50% of a given dose of disopyramide is excreted in the urine as the unchanged drug, about 20% as the mono-N-dealkylated metabolite and 10% as the other metabolites.

Pregnancy & Breastfeeding use

Pregnancy: There are no adequate and well-controlled studies in pregnant women. Lispine should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Lactation: Because of the potential for serious adverse reactions in nursing infants from Lispine, a decision should be made whether to discontinue nursing or to discontinue the drug , taking into account the importance of the drug to the mother

Contraindication

Lispine is contraindicated in the pre-existing A-V heart block, shock, glaucoma, urinary retention and known hypersensitivity to the drug.

Acute Overdose

Deliberate or accidental over dosage of oral Lispine may be followed by apnea, loss of consciousness & loss of spontaneous respiration. In such a case immediate hospitalization and all life saving measures should be taken.

Innovators Monograph

You find simplified version here Lispine

Lispine contains Disopyramide see full prescribing information from innovator Lispine Monograph, Lispine MSDS, Lispine FDA label

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