Primidon Holsten
Primidon Holsten Uses, Dosage, Side Effects, Food Interaction and all others data.
Primidon Holsten is an anticonvulsant used to treat essential tremor as well as grand mal, psychomotor, and focal epileptic seizures. Primidon Holsten was developed by J Yule Bogue and H C Carrington in 1949.
Primidon Holsten was granted FDA Approval on 8 March 1954.
Primidon Holsten alters sodium and calcium channel transport, reducing the frequency of nerve firing, which may be responsible for its effect on convulsions and essential tremor. Primidon Holsten 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.
| Trade Name | Primidon Holsten |
| 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 | Germany, Latvia |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Primidon Holsten is an antiepileptic used to treat grand mal, psychomotor, and focal epileptic seizures.
Primidon Holsten 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.
Primidon Holsten 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 Primidon Holsten works
Primidon Holsten and its metabolites, phenobarbital and phenylethylmalonamide (PEMA), are active anticonvulsants. Primidon Holsten does not directly interact with GABA-A receptors or chloride channels but phenobarbital does. Primidon Holsten 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.
Primidon Holsten 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.
Primidon Holsten 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
Primidon Holsten 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 Tmax if 2-4h. A 500mg oral dose of primidone Reaches a Cmax of 2.7±0.4µg/mL with a Tmax of 0.5-7h. Data regarding the AUC of primidone is not readily available.
Half Life
The half life of primidone is 7-22h in adults, 5-11h in children, and 8-80h in newborns.
Clearance
Primidon Holsten is cleared at a rate of 30mL/min.
Elimination Route
Primidon Holsten is 72.9-80.6% recovered in urine.
Innovators Monograph
You find simplified version here Primidon Holsten
