VALPROATE - THE DRUG OF CHOICE

                    ACHIEVING EXTREMITIES IS A MYTH.

 

       VALPROATE - THE DRUG OF CHOICE 

                                  

                                                   -PRAJWAL SIDRAMPURMATH

The above mentioned quote even applies for this so called Drug of Choice - VALPROATE.

INTRODUCTION :

No introduction will be that satisfactory since it is a drug with the most wide spectrum actions, effects, drug interactions, even a lot of adverse drug reactions/side effects.

Keeping the introduction brief, let’s directly jump into knowing about this amazing contribution that has changed the views of treating the disorders of personality etc.

 

 

MECHANISM OF ACTION :

1. ·         Primarily was discovered as a CALCIUM CHANNEL BLOCKER  (CCB).
2. ·         Also a SODIUM CHANNEL BLOCKER.
3. ·         Increases the GABA concentration in the synapses by two mechanisms : 1.increses the GABA synthesis. 2.decreases the metabolism of GABA.
4. ·         A minor role of inhibiting HISTONE DEACTYLASE.

MNEMONIC : C  Sachin  and  Ganguly  Hitting big sixes.

 

NOTE : We know that the drug is used mainly on what’s it’s action is, but it is worthy to remember that the side effects of particular drug also majorily depends on the other non-interested actions of the drug.

 

 

USES :

As you see the ,title VALPROATE – THE DRUG OF CHOICE, it’s a 1^st line drug in many clinical issues.

Like,   EPILEPSIES, MOTOR AND PERSONALITY DISORDERS. With the dose of anti-convulsants, there’s even little sedation is appreciated.

EPILEPTIC USES:

• 1.       Generalized tonic clonic seizures.
• 2.       Juvenile myoclonic epilepsy.
• 3.       Absence seizures.

NON EPILEPTIC USES:

• 4.       Lennox Gastaut Syndrome (LGS) – it’s a kind of mixed seizures and usually refractor, mainly seen in children.
• 5.       RAPID CYCLERS – bipolar disorder with >4 episodes of mania /depression per year.
• 6.       Rheumatic chorea.
• 7.       Acute mania: usually lithium is used as a preferred drug, but in cases of resistance to lithium, supplementation of valproate is proven to efficacious. And relatively higher oral doses of valproate is even superior to lithium as monotherapy.
• 8.      Proven effective in hair fall treatment with certain minerals (zinc), but this use is usually recommended, since as it's side effect there's a loss patchy hair loss [Alopecia].

Valproate is also used to treat – Acute Mania and last line drug in Migraine Prophylaxis.

 

 

ADVERSE DRUG REACTIONS/ SIDE EFFECTS :

Due to the following reasons even though a better drug it is not used in some lighter disorders like Migraine. As mentioned earlier achieving extremities is a myth.

1. ·         Alopecia – a sudden hair loss (patchy loss).
2. ·         Obesity.
3. ·         Polycystic ovary syndrome ( PCOS ).
4. ·         Some of its metabolites are hepatotoxic and their formation is induced by few drugs like – Phenytoin, Carbamazepine.
5. ·         Pancreatitis, Hyperammonemia, Tremors.
6. ·         Most common are – NAUSEA and VOMITTING.

 

DRUG INTERACTIONS :

May increase the plasma concentrations of few drugs like – Phenobarbitone and Lamotrigine (inhibits their metabolism), also Phenytoin (displaces it from bound state).

 

CONTRAINDICATIONS :

• 1.       Pregnancy – it causes Neural Tube Defects and few CVS defects. In cases of pregnancy that is presented and already on valproate, neither stop nor change the drug even fetotoxic because it may precipitate into status epileticus, so in such cases TDM is done, and a regular folate supplementation is advised i.e., 400 microgram/day.
• 2.       In children below 2 years of age – since liver is not mature enough to handle it’s toxic metabolites.

 

To conclude it’s always a discovery that changes things, try re-discovering yourselves in between the extremities (since none is perfect or imperfect).

EDIT: ALL YOUR FEEDBACKS ARE HEARTLY WELCOMED, AND A SPECIAL THANKS FOR PROVIDING YOUR VALUABLE FEEDBACK.