Kap Pharm CNS drugs

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What is the significance of glutamic acid in the CNS?: excitatory via increase influx of cations (direct coupling)
What is the main glutamic acid receptor in the CNS?: NMDA receptor
What are the drugs that are the main blockers of the NMDA receptor for glutamate?: ketamine and PCP
What are the receptors for GABA and what is the effect of each?: GABA A receptor = increase Cl influx
GABA B receptor = increse K efflux
(both via direct coupling)
What is the significance of GABA?: inhibitory via increased Cl influx or K efflux and the activities of GABA are increased by anticonvulsants, sedatives, hypnotics, and muscle relaxants
What is the main ACh receptor in the brain and what is it's mechanism? Second most common in brain?: M1 excitatory - decreases K efflux via DAG
M2 inhibitory - increased K efflux via cAMP
What is the main Nicotinic receptor in the brain and what is it's mechanism of action?: N excitatory - Na influx - direct coupling)
What are the main drugs given for alzheimers? Parkinsons?: Alzheimer's - AChE inhibitors
Parkinsons - M-blockers
What is the significance of dopamine? types of receptors how effected by CNS stimulants, anti-PD drugs, and antipsychotics?: inhibitory, multiple subtypes - G-protein linked to cAMP
- activity increases by CNS stimulants and anti-PD drugs,
- decreases by antipsychotics
what is the significance of norepinephrine?: excitatory or inhibitory via 2nd messengers and it is it is effected by stimulants, antidepressants, and anxiolytics
Where are most of the serotonin receptors located? What is the receptor action?: raffe nucleus
-stimulatory or excitatory, depending on receptor subtype
-receptors for all subtypes are 2nd messenger excepts for 5HT3.
What is the mechanism of opioid peptide receptors?: inhibitory, several subtypes - 2nd messenger coupling
-modified by opioid analgesics
What are the two main benzodiazepines? Barbiturate? Alcohol?: alprazolam, diazepam
Barbiturate: phenobarbital
alcohol: ethanol, chloral hydrate
How do benzodiazepines effect the Cl channel? barbituates?: Benzodiazipines:increase frequency
Barbituates: increase duration
What does the GABA-A receptor activation result in?: increased Cl ion influx leading to hyperpolarization (inhibitory)
Which drug acts as a benzodoazipine antagonist?: flumazenil, only effects benzodiazipine sites, not barbitue or ethanol sites
Why are barbituates more lethal than benzodiazepines at high levels?: they are able to open Cl channels and block Na channels (on their own) at high doses
What are the types of BZ receptors and what is the role of each?: BZ1 receptors - hypnotic actions
BZ2 receptors - role in memory, sensori-motor and cognitive functions
What is a drug that, although not a BZ, preferentially binds to the BZ1 receptor?: zolpidem
you know that it is not a Benzodiazipine, because a BZ will bind to any BZ receptor
What type of amnesia are benzodiazepines assoc. with?: anterograde amnesia (date rape drugs)
What are the first letters for the BZ which are metabolized outside the liver, and are not active metabolites?: OTL
Which BZ are used to treat anxiety states?: alprazolam, diazepam
Which BZ are used to treat sleep disorders?: triazolam
Which BZ are used to treat seizure states?: lorazepam
Which BZ are used to treat anesthesis?: midazolam
What is a unique feature concerning the metabolism of barbituates?: they are strong inducers of P450, and thus have many drug interactions
What are two non-BZ that activate BZ1 receptors and are used in sleep disorders? -how are they differens than BZs?: zolpidem and zaleplon

-bind only to BZ1 and less tolerance and thus less abuse than BZs
What is a drug that is not a BZ or barb and it's sole use is as an anxiolytic?: Buspirone
What is the mechanism of buspirone?: partial agonist of 5HT1A receptors (we don't know if it is stimulating or inhibiting)
What are some advantages and disadvantages of buspirone?: Non-sedating, no additive CNS depression with other drugs, No dependence liability

Very slow onset - might have to be given a couple weeks to see effects
What is important to know about dependence with Sedative hypnotic drugs?: chronic use leads to tolerance - in case of BZs via down regulation of BZ receptors

Psychological and physical dependence occur - especially with barbs and ethanol

Rebound REM sleep, insomnia, and anxiety are common on discontinuance

With ethanol and short acting barbs this withdrawal can lead escalate to anxiety, agitation, hyperreflexia, and seizures
How do you treat severe withdrawal symptoms?: give another similar drug, usually a long acting BZ and taper the dose
Which drug inhibits acetaldehyde dehydrogenase and what is it's function?: disulfiram

inhibits acetaldehyde dehydrogenase (used in metabolism of ethanol) and thus there is a buildup of acetaldehyde. this buildup of acetaldehyde makes the drinker very sick and thus it is sometimes used for people who want to quit drinking
What are the three mechanisms of action of anticonvulsants?: increase inhibitory tone via GABA mediated hyperpolarization

decrease axonal conduction by blocking fast Na channels

decrease presynaptic Ca influx through the T channels in talamic neurons

decrease excitatory effects of glutamic acid
Which drugs act by increasing inhibitory tone by facilitation of GABA-mediated hyperpolarization: barbiturates, benzodiazepines
Which drugs act via decreasing axonal conduction by blocking fast Na channels: phenytoin, carbamazepine
(high dose barbiturates and valproic acid)
which drugs decrease presynaptic Ca influx through type T channels in thalamic neurons?: ethosuximide and valproic acid
Which drugs decrease excitatory effects of glutamic acid?: lamotrigine and topiramate (blocks AMPA receptors)

felbamate (blocks NMDA receptors)
What are the main drugs given for Partial (simple or complex) seizures? backup drugs?: valproic acid, phenytoin, carbamazepine

backup: Phenobarbital in pregnancy
What are the drugs of choice in General - tonic-clonic seizures? backup drugs?: Valproic acid, phenytoin, carbamazepine

backup: phenobarbital in pregnancy
What are the drugs of choice for general absence seizures? backup drugs?: Ethosuximide, valproic acid, clonazepam

backup - Lamotrigine
What are the drugs of choice for general myoclonic seizurse? backup drugs?: valproic acid

backup - clonazepam, felbamate
What are the drugs of choice for status epilepticus seizures? backup drugs?: Lorazepam, diazepam, phenytoin, or forphenytoin

backup: phenobarbital (long term)
What is the mechanism of phenytoin: blocks axonal Na channels in inactivated state (state dependent blockade)
What are two other uses of phenytoin other than as an anticonvulsant?: class IB antiarrythmic and backup for Bipolar disorder
What are the important facts about the absorption of phenytoin?: Variable oral absorption and first-pass metabolism

competetion for protein binding and increased P450 cause drug interactions
What are the adverse effects of phenytoin?: sedation, acne, gingival overgrowth, hirsutism, osteomalacia, hematotoxicity
Is phenytoin teratogenic?: yes, it causes Fetal Hydantoin syndrome which includes structural abnormalities such as cleft palate and cleft lip.
What is the mechanism of action for Carbamazepine?: Mechanism like phenytoin
What is Carbamazepine the drug of choice for and what is it a back up for?: DOC: trigeminal neuralgia

Back up: Bipolar disorder
What is important about hte metabolism of carbamazepine?: it induces P450
What are the adverse effects of carbamazipine?: sedation, osteomalacia, hematotoxicity granulocytopenia, anemia, water retention do to increased ADH, dermatitis
Is carbamazepine teratogenic?: yes, it causes craniofacial abnormalities
Which of the anticonvulsants is notorious for causing spina bifida?: valproic acid
What is the mechanism of action of Valproic acid?: multiple actions including block of T-type Ca channels, inhibition of
GABA transaminase and block of Na channels
What is important about the metabolism of valproic acid?: Inhibits P450 (ulike phenytoin or carbamazapine)
Other than being an anticonvulsant, what are other uses of valproic acid?: backup in bipolar and used in migrains
What are the adverse effects of valproic acid?: GI tract and liver toxicity due to toxic metabolite
Is valproic acid teratogenic?: yes, SPINA BIFIDA
What is the mechanism for ethosuximide?: Blocks T-type Ca channels.
What are the uses of ethosuximide?: absence seizures are sole use
What are the adverse effects of Ethosuximide?: Strong GI distress
Is ethosuximide teratogenic?: No, it is safe in pregnancy.
Of the barbiturates and benzodiazepines, which drug has anti-seizure activity at low doses and a long half life?: phenobarbital
Of the barbiturates and benzodiazepines, which drug is usually a backup due to marked sedation?: clonazepam
Of the barbiturates and benzodiazepines, which drug is used IV in status epilepticus?: Lorazepam and diazepam
What is the anticonvulsnat which is most known for severe skin reactions?: lamotridine
Which anticonvulsant is useful in neuropathic pain??: gabapentin
What are the newer anticonvulsant drugs?: felbamate, gabapentin, lamotrigine
What are the general features of anticonvulsant drug use?: Additive CNA depression with other drugs

avoid abrupt withdrawal which may precipitate seizures

DECREASED EFFICACY OF ORAL CONTRACEPTIVES and other drugs also
What is the barbituate used for hypnonis (sleep)?: secobarbital
What is the barbituate used for seizure states?: phenobarbital
What is the barbiturates used as a short acting IV anesthetic?: thiopental

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