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Golden Points


Drugs For Central Nervous System Diseases

  1. Benzodiazepines are MC used sedatives and hypnotics. These are GAMA facilitory drugs. Diazepam is MC used sedative & hypnotic with t\1\2-100; it is DOC for status epileptics, febrile seizures, drug induced hyperactivity, picrotoxin poisoning, prevention of seizures due to lidocaine, emergence deliverium due to ketamine, drug induced EPS or excitement of mania-flumazenil is antidote of diazepam
  2. LEO (Lorazepam, Estazolam, Oxazapam) are water-soluble benzodiazepines and are metabolized outside liver.
  3. Benzodiazepines cause anterograde amnesia (head injury causes retrograde amnesia).
  4. Cholordiazepoxide (high dose) is DOC for alcohol withdrawal from alcohol; diazepam is however for delirium tremons.
  5. Flunitrazepam is date rape drug; chloral hydrate (dry wine), ketamine and GHB are other drugs for same purpose.
  6. Phenytoin acts by inhibiting depolarizing shift in neurons; MC side effect is gum hyperplasia; others are hirsutism, hypocalcemia, Osteomalacia, megaloblastic anemia (do MCV testing), pseudolymphoma and hypersensitivity (discontinue the drug)
  7. Carbamazepine is DOC for all kind of neuralgias (trigeminal\glossopharyngeal) & partial seziure; MC side effect is rash (10%), leukopenia and hepatitis
  8. Valproic acid is broadest spectrum antiepelipetic drug; DOC for GTCS, akinetic, atonic, myclonic & mixed epilepsies; causes hepatoxtocity mainly in children, weight gain
  9. Phenobarbitone is CI in acute intermittent porphyria; DOC for hemolytic anemia, jaundice in newborn, epilepsy following febrile seizures, & epilepsy in pregnancy
  10. Buspirone is a non-sedative anxiolytic drug (5HT1A partial agonist) that is devoid of properties possessed by diazepam such as muscular relaxation, amnesia, sedation, anti-convulsant action etc. Its main drawback is that it takes two weeks to start its action therefore is used in maintenance of patients with generalized anxiety disorders rather than in acute phase
  11. Thiopentone is highly lipid soluble (MC inducing agent), barbiturate that undergoes redistribution
  12. Donepazil is the DOC for Alzhiemer’s disease, a organic brain disease (MC cause of dementia); occurs due to acetylcholine deficiency
  13. Levodopa is most effective anti-parkinson drug, only drug that lowers mortality
  14. Amantidine (also an antiviral drug-Influenza A2) enhances dopamine transmission (MC side effect is ankle edema)-CI in renal failure and epilepsy.
  15. Tolcapone and entacapone are COMT inhibitors and are used in severe Parkinson’s disease. Tolcapone can cause hepatic failure but is more potent.
  16. Morphine was isolated by Serturner from poppy plant it is analgesic and antitussive
  17. Pethidine is synthetic opioid that has anticholinergic property (causes mydriasis) while other opioids cause meiosis
  18. Pethidine gets accumulated in renal failure causing hyperreflexia; this is known as norpethidine syndrome
  19. Buprenorphine is the longest acting opioid that has alcohol anti-craving properties (methadone is DOC for opioid detoxtification). Importantly, buprenorphine binds to mu receptors so tightly that even morphine is not able to reverse its actions.
  20. Naloxone (most potent opioid antagonist) doesn’t reverse the overdose of Bwuprenorphine due to its ceiling effect
  21. Morphine is DOC for acute pulmonary edema, Tetralogy of Fellot’s
  22. Opioids don’t have anti-inflammatory properties but are useful in severe pain of visceral origin as they work by reducing the release of substance P from spinal cord’s substantia gelatinososa
  23. Histamine’s maximum amount is found in lung mast cells (90% of body’s histamine is present there)
  24. Astemazole is longest acting newer antihistaminic and citirizine, although a member of newer non-sedative family; out of newer drugs it produces maximum sedation
  25. Older anti-histaminics are better for urticaria and itching due to their anticholinergic effects while newer ones are better for sneezing and common cold etc
  26. Fexofenadine (Allergra), a newer analogue of hepatotoxic and cardiotoxic drug terfenadine is not associated with torsa de depointes
  27. Citirizine is a metabolite of Promethazine but is devoid of sedative effect at usual therapeutic doses (in some it produces sedation)
  28. Promethazine (phenargan) is DOC for drug induced extrapyramidal disturbances
  29. Sumatriptan, a 5-HT1b\1d partial agonist is the DOC for acute attack of migraine; propranolol is DOC for prevention of migraine
  30. Sumatriptan can cause vasospasm, therefore is contraindicated in hypertension, angina and peripheral vascular diseases patients
  31. Alcohol is most prevalent neurotoxin in our environment
  32. Disulfiram (metronidazole has dilsulfiram like effect) has is alcohol dehydrogenase inhibitor and is DOC for alcohol detoxification. It is being studied for cocaine dependence as well. 
  33. Legal limit of alcohol is 80mg\dl in most nations and levels above 400mg\dl are uniformly fatal; it follows zero order kinetics (phenytoin, Tolbutamide, theophylline, warfarin, aspirin, caffeine) also follow zero-order kinetics (fixed amount is metabolized
  34. Ethylene glycol poisoning shows presence of oxalate crystals in urine
  35. Fomepizole\ethanol are DOC for methylalcohol poisoning (causes blindness due to optic atrophy)

Newer Drugs


Sodium oxybate (neurotransmitter)

Cataplexy associated with narcolepsy


Memantine (NMDA blocker)

Alzhiemer’s disease


Zolpedam\zopiclone\zaleplon (BZDA1 agonists)



Topiramate (Na +channel blocker; carbonic anhydrase inhibitor, GABAergic)

Antiepileptic, neuropathic pain; migraine prophylaxis


Zonisambide (Na+ channel blocker)

Antipileptic, neuropathic pain


Felbamate (Increase GABA, decrease Glutamate)

Lennox – Gastaut syndrome


Tiagabine (potentiates GABA)



Oxacarbazine (Na+channel blocker)



Trientine (Copper chelator)

Wilson’s disease


Ramelteon (Melatonin agonist)



Rimonabant (CB1 receptor blocker)



Telampenal (AMPA antagonist)

Anti-epileptic drug


Indiplon (Non-BZD)



Interferon 1 beta

Relapsing multiple sclerosis


Tetrabenazine (Monoamine depletor)

Huntington’s chorea


Rotigotine (New D1 analogue)

Non-ergoline used for PD


Armodafinil (single-isomer of modafinil)



Recent Advances:

Tafluprost : A fluorinated analog of PGF2á .Approved for reducing elevated intraocular pressure in patients with open-angle glaucoma by increasing uveoscleral outflow. It is used as ophthalmic solution .


Ezogabine (retigabine) : A potassium channel opener approved for adjunctive therapy for partial-onset seizures.


Asenapine: It is approved for the acute treatment of schizophrenia in adults and for the acute treatment of manic or mixed episodes associated with bipolar I disorder, with or without psychotic features, in adults.


Levetiracetam : Antiepileptic drug useful for partial seizures.


Mirtazapine : Newer antidepressant drug also known as nor-adrenergic and specific serotonergic antidepressant (NSSA). It acts by inhibiting presynaptic auto- and hetero-a2 receptors.

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