Prysoline

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

Prysoline is an anticonvulsant used to treat essential tremor as well as grand mal, psychomotor, and focal epileptic seizures. Prysoline was developed by J Yule Bogue and H C Carrington in 1949.

Prysoline was granted FDA Approval on 8 March 1954.

Prysoline alters sodium and calcium channel transport, reducing the frequency of nerve firing, which may be responsible for its effect on convulsions and essential tremor. Prysoline has a wide therapeutic window as doses of 50-1000mg/day were effective. Patients should be counselled regarding the risk of status epilepticus with abrupt cessation of primidone.

Prysoline
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Prysoline
Availability	Prescription only
Generic	Primidone
Primidone Other Names	2-deoxyphenobarbital, Primidon, Primidona, Primidone, Primidonum
Related Drugs	gabapentin, clonazepam, lamotrigine, diazepam, pregabalin, Lyrica, topiramate, levetiracetam, Keppra, Topamax
Type
Formula	C₁₂H₁₄N₂O₂
Weight	Average: 218.2518 Monoisotopic: 218.105527702
Protein binding	Primidone is 10.78-13.70% protein bound in serum.
Groups	Approved, Vet approved
Therapeutic Class
Manufacturer
Available Country
Last Updated:	September 19, 2023 at 7:00 am

Uses

Prysoline is an antiepileptic used to treat grand mal, psychomotor, and focal epileptic seizures.

Prysoline is commonly indicated for the management of grand mal, psychomotor, and focal epileptic seizures. In addition, it has also been studied and utilized as an effective management of essential tremor.

Prysoline is also used to associated treatment for these conditions: Grand mal Generalized tonic-clonic seizure, Partial-Onset Seizures, Temporal Lobe Epilepsy (TLE), Tremor, Essential

How Prysoline works

Prysoline and its metabolites, phenobarbital and phenylethylmalonamide (PEMA), are active anticonvulsants. Prysoline does not directly interact with GABA-A receptors or chloride channels but phenobarbital does. Prysoline alters transmembrane sodium and calcium channel transport, reducing the frequency of nerve firing, which may be responsible for the primidone’s effect on convulsions and essential tremor.

Toxicity

The oral LD₅₀ in rats is 1500mg/kg and in mice is 280mg/kg. The intraperitoneal LD₅₀ in rats was 240mg/kg and in mice was 332mg/kg.

Patients experiencing a primidone overdose may present with CNS depression, coma, respiratory depression, suppressed reflexes, suppressed response to pain, hypotension, and decreased urine output. Overdose should be treated with symptomatic and supportive treatment, including the removal of unabsorbed drug.

Food Interaction

Avoid alcohol.
Avoid St. John's Wort.

Prysoline Alcohol interaction

[Major] GENERALLY AVOID:

Concurrent acute use of barbiturates and ethanol may result in additive CNS effects,

including impaired coordination, sedation, and death.

Tolerance of these agents may occur with chronic use.

The mechanism is related to inhibition of microsomal enzymes acutely and induction of hepatic microsomal enzymes chronically.

The combination of ethanol and barbiturates should be avoided.

Prysoline Drug Interaction

Moderate: duloxetine, escitalopram, atorvastatin, pregabalin, metoprolol, metoprolol, montelukast, levothyroxine, acetaminophen, cholecalciferolUnknown: aspirin, aspirin, rosuvastatin, omega-3 polyunsaturated fatty acids, fluticasone nasal, furosemide, tiotropium, budesonide / formoterol, cyanocobalamin, ascorbic acid

Prysoline Disease Interaction

Major: acute alcohol intoxication, drug dependence, porphyria, rash, respiratory depression, phenobarbital metabolite 1, renal/liver diseaseModerate: suicidal tendency, adrenal insufficiency, depression, hematologic toxicity, osteomalacia, paradoxical reactions, phenobarbital metabolite 2

Volume of Distribution

The volume of distribution of primidone is 0.5-0.8L/kg.

Elimination Route

Oral primidone is up to 80% bioavailable with a T_max if 2-4h. A 500mg oral dose of primidone Reaches a C_max of 2.7±0.4µg/mL with a T_max of 0.5-7h. Data regarding the AUC of primidone is not readily available.