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.

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
Prysoline
Prysoline

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.

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

Prysoline is cleared at a rate of 30mL/min.

Elimination Route

Prysoline is 72.9-80.6% recovered in urine.

Innovators Monograph

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https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8412
http://www.hmdb.ca/metabolites/HMDB0014932
http://www.genome.jp/dbget-bin/www_bget?drug:D00474
http://www.genome.jp/dbget-bin/www_bget?cpd:C07371
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=4909
https://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46507775
https://www.chemspider.com/Chemical-Structure.4740.html
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50248152
https://mor.nlm.nih.gov/RxNav/search?searchBy=RXCUI&searchTerm=8691
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=8412
https://www.ebi.ac.uk/chembldb/index.php/compound/inspect/CHEMBL856
https://zinc.docking.org/substances/ZINC000000001979
http://bidd.nus.edu.sg/group/cjttd/ZFTTDDRUG.asp?ID=DAP000678
http://www.pharmgkb.org/drug/PA451105
http://www.rxlist.com/cgi/generic2/primid.htm
https://www.drugs.com/cdi/primidone.html
https://en.wikipedia.org/wiki/Primidone
*** Taking medicines without doctor's advice can cause long-term problems.
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