IV - Topnotch Pharma Flash Cards - CNS Drugs
bind GABA-A receptor subunits to increase frequency of chloride channel opening which causes membrane hyperpolarization
benzodiazepines (TOPNOTCH)
SE: anterograde amnesia, decreased psychomotor skills, unwanted daytime sedation, tolerance, dependence liability and rebound insomnia or anxiety
benzodiazepines (TOPNOTCH)
BZD that can be used for seizure disorders, Bipolar disorder and infantile spasm
Clonazepam (TOPNOTCH)
Why is Lorazepam preferred over Diazepam in status epilepticus
due to its long distribution halflife (TOPNOTCH)
date-rape drug
Flunitrazepam (TOPNOTCH)
BZD used for alcohol withdrawal
Diazepam and Chlordiazepoxide (TOPNOTCH)
antagonist at benzodiazepine sites on GABA-A receptor
Flumazenil (TOPNOTCH)
bind to GABA-A receptor sites to increase duration of chloride channel opening, block glutamic acid neurotransmission
barbiturates (TOPNOTCH)
which has greater dependence liability: barbiturates or benzodiazepine
barbiturates (TOPNOTCH)
Barbiturate with the highest lipid solubility
Thiopental (TOPNOTCH)
barbiturate for status epilepticus
Phenobarbital (TOPNOTCH)
SE: acute intermittent porphyria
barbiturates (TOPNOTCH)
High dose BZD and Barbs may suppress seizure but at the expenses of marked sedation EXCEPT for
Clonazepam and Phenobarbital (TOPNOTCH)
only interact with GABA-A receptors with alpha-1 subunit; For insomnia and sleep disorder esp when sleep onset is delayed
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
dependence liability and withdrawal symptoms is less than that of benzodiazepines
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
lack anti-convulsant, anti-anxiety and muscle relaxant effects, effects are reversed with Flumazenil, very rapid onset of action, may dec REM sleep
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
increasing use due to rapid onset with minimal effects on the sleep pattern and cause less daytime cognitive impairment as compared to BZD
Zolpidem, Zaleplon, Eszopiclone (TOPNOTCH)
partial agonist at 5-HT1A receptors and possibly D2 receptors, used For generalized anxiety disorders
Buspirone (TOPNOTCH)
slow onset of action (more than 1week), metabolized by CYP3A4, safe for pregnant patients
Buspirone (TOPNOTCH)
activates melatonin receptors (MT1 and MT2 receptors) in the suprachiasmatic nuclei in the CNS leading to dec latency of sleep onset
Ramelteon (TOPNOTCH)
block voltage-gated Na channel; DOC for generalized tonic-clonic seizures, DOC for partial seizures, can be used for migraine
Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)
SE: nystagmus, diplopia, sedation, gingival hyperplasia, hirsutism, anemias, peripheral neuropathy (absent DTRs), osteoporosis, fetal hydantoin syndrome, abnormalities in Vit D metabolism
Phenytoin, Fosyphenytoin, Mephenytoin, Ethotoin (TOPNOTCH)
preferred in prolonged therapy for status epilepticus because it is less sedating
phenytoin (TOPNOTCH)
block voltage-gated Na channels and decreases glutamate release; DOC for trigeminal neuralgia, DOC for generalized tonic-clonic seizures, DOC for partial seizures, for bipolar disorders
Carbamazepine, Oxcarbazepine (TOPNOTCH)
SE: diplopia, cognitive dysfunction, drowsiness, ataxia, blood dyscrasias, Stevens-Johnson syndrome, erythematous rash, teratogen (spina bifida and craniofacial anomalies), hyponatremia
Carbamazepine, Oxcarbazepine (hyponatremia) (TOPNOTCH)
may be used for acute manic phase and as prophylaxis in the depressive phase
Carbamazepine, Oxcarbazepine (TOPNOTCH)
blocks high-frequency firing of neurons which modifies amino acid metabolism; DOC for bipolar disorder (acute mania), DOC for generalized tonic-clonic seizures and absence seizure, partial seizures, myoclonic seizures, also used for Bipolar disorders
Valproic acid (TOPNOTCH)
anti-manic that is CYP450 inhibitor
Valproic acid (TOPNOTCH)
for status epilepticus in children ; primary anticonvulsant in infants, children and pregnant patients
Phenobarbital (TOPNOTCH)
inhibit low threshold (T-type) Ca currents esp in thalamic neurons ; DOC for absence seizure
Ethosuximide, Phensuximide, Methsuximide (TOPNOTCH)
blocks Ca channels, increases GABA release ; For neuropathic pain such as postherpetic neuralgia, partial seizures, migraine
Gabapentin, Pregabalin (TOPNOTCH)
structural analogues of GABA but does not activate GABA receptor directly ; also have the same effect on Ca currents like Ethosuximide
Gabapentin, Pregabalin (TOPNOTCH)
blocks Na and Ca channels and decreases glutamate, used for acute manic phase and as prophylaxis in the depressive phase
Lamotrigine (TOPNOTCH)
primarily undergoes glucuronidation reaction ; SE: dizziness, ataxia, nausea, rash, SJS / TEN
Lamotrigine (TOPNOTCH)
Bind synaptic protein selectively inhibiting hypersynchronization of epileptiform burst firing ; For generalized tonic-clonic seizures, partial seizures
Levetiracetam (TOPNOTCH)
not metabolized by CYP450 enzymes, eliminated in the kidneys in their unchanged form
Levetiracetam (TOPNOTCH)
multiple actions on synaptic function, probably via actions on phosphorylation (Na, Ca, GABA, AMPA-glutamate, carbonic anhydrase)
Topiramate, Felbamate (TOPNOTCH)
also facilitate the inhibitory actions of GABA but its exact MOA is still unknown
Felbamate (TOPNOTCH)
Antiseizure drugs with the most number of MOA, undergo both hepatic and renal metabolism
Topiramate, Felbamate (TOPNOTCH)
Irreversibly inactivates GABA aminotransaminase (GABA-T) which terminates the action of GABA ; For GTC seizure
Vigabatrin (TOPNOTCH)
Inhibits GABA transporter (GAT-1) in neurons and glia thus inhibiting its reuptake, leading to prolongation of GABA effects ; For partial seizures
Tiagabine (TOPNOTCH)
SE: visual field defects
Vigabatrin (TOPNOTCH)
Facilitates GABA-mediated inhibition, block brain NMDA and Ach-N receptors
Inhalational anesthetics (TOPNOTCH)
SE: megaloblastic anemia on prolonged exposure; Euphoria (laughing gas), bronchodilation
Nitrous Oxide (TOPNOTCH)
Lowest Potency (highest MAC) and least cardiotoxic
Nitrous Oxide (TOPNOTCH)
all inhaled anesthetcis cause bronchodilation except
Desflurane (TOPNOTCH)
SE: catecholamine-induced arrhythmias, peripheral vasodilation, bronchodilation
Isoflurane (TOPNOTCH)
SE: spike-and-wave activity in EEG, muscle twitching, breath-holding, myocardial depression, renal insufficiency (due to Flourine release), dec cardiac output, bronchodilation
Enflurane (TOPNOTCH)
has pungent odor which limits its use
Enflurane (TOPNOTCH)
SE: catecholamine-induced arrhythmias, myocardial depression, post-operative hepatitis, dec cardiac output, bronchodilation
Halothane (TOPNOTCH)
Highest potency and lowest MAC (very slow onset and recovery)
Methoxyflurane (TOPNOTCH)
a usual adjunct with inhalational anesthetics and IV opioids, has a slow onset but longer DOA
Midazolam (TOPNOTCH)
Blocks excitation by glutamate at NMDA receptors; For dissociative anesthesia (analgesia, amnesia and catatonia but with retained consciousness)
Ketamine (TOPNOTCH)
congener of Phencyclidine / angel dust
Ketamine (TOPNOTCH)
For general anesthesia to patients with limited cardiac or respiratory reserve
Etomidate (TOPNOTCH)
Interacts with mu, sigma, kappa receptors for endogenous opioid peptides ; For high risk patients who might not survive general anesthesia
Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)
SE: respiratory depression, chest wall rigidity (which may cause impaired ventilation) and constipation
Opioid analgesics: Fentanyl, morphine, alfentanil, remifentanil (TOPNOTCH)
Antidote is Naloxone / Naltrexone
Opioid toxicity (TOPNOTCH)
milk of anesthesia
Propofol, Fospropofol (TOPNOTCH)
Potentiates GABA-A receptors, blocks Na channels; For prolonged sedation esp in ICU patients and also in OPD surgeries
Propofol, Fospropofol (TOPNOTCH)
Blockade of Na channels slows which prevents axon potential propagation
Local Anesthetics (TOPNOTCH)
Shortest half-life among local anesthetics
Procaine (TOPNOTCH)