CNS drugs Flashcards by Adam Killpack

chlorpromazine**

→ block D2, α-adrenergic, antihistamine & considerable anticholinergic; Jaundice
neg. ionotrpic on heart
(low potency) →↑-

How well did you know this?

Not at all

Perfectly

Thioridazine

retinal deposits
Chorpromazine→ block D2, α-adrenergic, antihistamine & considerable anticholinergic; Jaundice
neg. ionotrpic on heart
(low potency)

How well did you know this?

Not at all

Perfectly

Fluphenazine

→ more selective for dopamine, less anticholingeric, ↑ extrapyramidal effects
(high potency)

How well did you know this?

Not at all

Perfectly

Perchloroperazine

Phenothiazine

→ nausea & vomiting

How well did you know this?

Not at all

Perfectly

Trifluoperazine

→ less anticholinergic: ↑ extrapyramidal, ↓ hypoTN & sedation

How well did you know this?

Not at all

Perfectly

Haloperidol**

→ greater potency at D2, some α1 & 5HT2, no anticholinergic; MOST likely to cause pyramidal

used for acute psychotic situations;
tourettes

How well did you know this?

Not at all

Perfectly

Pimozide

→ binds ONLY to D2; high extrapyramidal, mod. antichol;

Tourettes syn tics

-prolong QT (risperidone, ziprasidone, pimozide)

How well did you know this?

Not at all

Perfectly

Loxapine

→ use when others dont work; greater seizure risk than Phenothiazines

How well did you know this?

Not at all

Perfectly

Olanzapine**

blocks D2, D4* (+ symp), 5-HT2a (neg. symp); anti-ACh (↓ ↓ extrapyramid); (anti-Hist/ACh/alpha 1)
tx Bipolar
→ WEIGHT GAIN (most likely)
(first line drug)

How well did you know this?

Not at all

Perfectly

Risperidone*

→ inhib D2 & esp 5HT2a; block α; +SSRI for resitant depression & autism (↑ DA in basal gang)

Plaiperidone is metabolite
-prolong QT (risperidone, ziprasidone, pimozide)
(first line drug)

How well did you know this?

Not at all

Perfectly

Ziprasidone*

→ similar to risperidone; 5HT1a agonism or inhabit 5HT repute

tx Tourette, acute mania;
-prolong QT (risperidone, ziprasidone, pimozide)
↓ chance weight gain; hyperprolactinemia
-caution w/ pts who have history of seizures

How well did you know this?

Not at all

Perfectly

Clozapine

→ binds D4 & 5HT2a > affinity than D2 (↓↓ extrapyramidal) binds α1 & histamine & anti-ACh;

agranulocytosis; RESERVED;
psychosis in Parkisons pts

How well did you know this?

Not at all

Perfectly

Quetiapine*

→ similar to clozapine; ↑ + & - symp; ↓ ↓ SE;

**-↑ NE via metabolite & 5-HT2c block
-little Prolactin affect
-monotherapy for bipolar
first line drug

How well did you know this?

Not at all

Perfectly

Iloperidone

→ block D2 & 5HT2a, α1; no muscarinic

How well did you know this?

Not at all

Perfectly

Lurasidone

→ block D2 5HT2a, partial agonist 5HT1a; NO antihistamine or muscarinic; agranulocytosis & neutropenia

How well did you know this?

Not at all

Perfectly

Asenapine

→ blocks 5-HT2a & 2c, D3** (not strong D2);

blocks histamine & α (not muscarinic)
tx: PTSD nightmares

-less metabolic effects

How well did you know this?

Not at all

Perfectly

Aripiprazole**

→ dopamine stabilizer;

partial agonist @ D2 & 5-HT1a;
blocks 5HT2a, α1, & histamine
no affect on prolactin, QT;
less weight gain.

SE- ↓ esophageal motility (aspiration pneumonia)
↑ blood glucose (diabetes may develop or worsen)

How well did you know this?

Not at all

Perfectly

Lithium**

→ ↓ release & turnover of NE & DA;

↑ ACh;
↓ IP3 and DAG
may uncouple receptors from G-protein (hypothyroid & polyuria)
SLOW onset of action
prevent mania and depression

-competes w/ Na in proximal tubule for reabsorption

↓ Lithium clearance:

-low Na
-Thiazide diuretics
-NSAID

SIDE EFFECTS

TREMOR (tx w/ βB)
Nausea
Headache
↓ thyroid function (blocks thyroxine)
Renal effects- nephrogenic diabetes insipidus (tx: amiloride)
weight gain

How well did you know this?

Not at all

Perfectly

Divalproex

Valproic Acid

→ blocks Na, ↓ NMDA receptor stim, ↑ GABA synthesis & lvls
-DOC if both seizure types occur together (can be used for all seizure types except infantile spasm);

-LIVER toxicity, pancreatitis; hair loss
several drug interaction

BIPOLAR
→ anticonvulsant; effect >= Lithium; rapid onset;
pts who dont respont to Li; few SE

category D

How well did you know this?

Not at all

Perfectly

Phenytoin**

Fosphenytoin

→ prolong inactivation of Na channel (prevents spread & inhibits glutamate release)
-no general CNS depression, not very sedating
-Zero order metabolism at therapeutic levels
-↑ [warfarin] (↓metabolism)
-↑ metabolism of oral contraceptives
LOTS OF SE & INTERACTIONS

→ water soluble prodrug (IV use)

How well did you know this?

Not at all

Perfectly

Carbamazepine**

→ blocks Na & inhibits NTM (glutamate) release; inhib NE release & reuptake;
-mood stabilizing (bipolar)
-Idosyncratic blod dyscracias:
--aplastic anemia 
--agranulocytosis
--mild leukopenia
(mainly in elderly for trigem)

DOC for partial seizures;
1st drug for tonic-clonic seizures, Trigeminal nerualgia (↑ doses)

How well did you know this?

Not at all

Perfectly

Levatiracetam*

ANTICONVULSANT
→ binds SV2A (↓ glutamate & ↑ GABA); few drug interactions
-Partial & generalized tonic-clonic seizures
-Myoclonic seizures

How well did you know this?

Not at all

Perfectly

Lamotrigine*

ANTICONVULSANT
→ inactivates Na, N & P/Q Ca++ channels (absence seizures), ↓ glutamate;
-Dermatitis (life-threatening in children)

–Partial & generalized tonic-clonic seizures

Atonic seizures
category C

How well did you know this?

Not at all

Perfectly

Topiramate**

ANTICONVULSANT
→ block Na channels, ↑ GABAa current, ↓ glutamate receptor activation;
-inhibits SPREAD not ↑ threshold;
-secreted unchanged in urie

treatment for:

-bipolar
-eating disorder & binge eating
-weight loss aid
-alcoholics (started in teens)

-SE acute myopia & glaucoma

Partial & generalized tonic-clonic seizures
infantile spasm

-helps ↓ craving in recovering alcoholics

category C

How well did you know this?

Not at all

Perfectly

Gabapentin

Pregabalin

ANTICONVULSANT
→ GABA analogs, not on receptors, ↑ GABA release; block N-type Ca+ (inhib glutamate release) TMJ
→ fibromyalgia

category C

How well did you know this?

Not at all

Perfectly

Vigabatrin

ANTICONVULSANT
→ irreversible inhib of GABA transaminase; ↑ GABA levels & tonic inhib of brain;

Irreversible constriction of visual field and/or retinal damage;

CI pre-exisitng mental illness

How well did you know this?

Not at all

Perfectly

Tiagabine*

ANTICONVULSANT
→ inhib. GABA uptake (forebrain & hippo);
–prolong inhib action of GABA

adjunt tx partial seizures

How well did you know this?

Not at all

Perfectly

Ethosuximide**

→ DOC for absence seizure; block T-type Ca channels; GI SE; valproic acid ↓ clearance

How well did you know this?

Not at all

Perfectly

Carbamazepine ↑ metabolism of

-phenytoin
-primidone
-ethosuximide
-valproic acid
-clonazepam
-haloperidol
-oral contraceptives

How well did you know this?

Not at all

Perfectly

↑ metabolism of Carbamazepine

-phenobarbital
-phenytoin
-valproic acid
-carbamazepine

How well did you know this?

Not at all

Perfectly

↓ Metabolism of Carbamazepine:

-Cimetidine
-Fluoxetine
-Isoniazid
-erythromycin

How well did you know this?

Not at all

Perfectly

Valproic acid ↓ metabolism of:

Valproic acid
Phenytoin (& displaces)
Carbamazepine
Phenobarbital (coma)
↓ elimination of lamotrigine

How well did you know this?

Not at all

Perfectly

Baclofen**

GABA-mimetic
→ GABAb agonist brain & spine; ↓ excitatory NTM;
-may ↓ substance P (↓ pain)
-intrathecal administration: better control

tx: chronic spascitiy, back pain, prevent migraines

How well did you know this?

Not at all

Perfectly

Diazepam**

→ GABAa in spinal cord; required dose causes significant sedation; spasm w/ trauma

How well did you know this?

Not at all

Perfectly

Cyclobenzaprine**

→ similar structure as TCA; sedative @ brain stem; anti-ACh;

significant sedation, confusion –transient visual hallucination
spasms from trauma/sprain;

How well did you know this?

Not at all

Perfectly

Carisoprodol

→ metabolite (meprobamate) is anxiolytic (acts like barbs); addiction potential; ↑ microsomal enz)

How well did you know this?

Not at all

Perfectly

Tizanidine**

→ analogue of clonidine; acts at α2; pre/post synaptic inhib;
-inhib pain @ dorsal horn;
-SEDATING 
hypoTN (esp w/ antHTN rx)
-dry mouth, muscle weakness (elderly)

How well did you know this?

Not at all

Perfectly

Dantrolene**

→ targets excitation contraction coupling not CNS;
-↓ Ca release from SR;

tx: malignant hyperthermia & neuroleptic malignant syndrome (antipsychotics)

How well did you know this?

Not at all

Perfectly

Methylphenidate

→ ADHD & narcolepsy; ↑ DA & NE in prefrontal ctx → modulate GABA & glutamate

How well did you know this?

Not at all

Perfectly

Amphetamine

→ ADHD & narcolepsy; ↑ DA & NE in prefrontal ctx → modulate GABA & glutamate

Atamoxetine**

→ SNRI, potentiate effects of β-agonists, dont use w/ vasopressors
Tx: ADHD in adolescents and children 6+

possible liver toxicity

Caffeine

→ blocks adenosine receptors & inhib PDE; ↑ contractility dilates coronary aa, constricts cerebral (headache tx) moderate bronchodilation, ↑ gastric acid, diuresis

Levodopa**

→ able to pass BBB; high doses needed b/c peripheral metabolism; nausea & vomitting esp. effective against bradykinesia; arrhythmias, htpoTN & HTN w/ MAOI, dyskinesia
-On/Off phenomenon

Carbidopa

→ dopa decarboxylase inhib, doesnt cross BBB; ↓ DA synthesis in periphery

Carbidopa/levodopa**

→ combo ↑ DA in brain & ↓ in periphery; ↓ nausea & vomiting; food ↓ aborp, taken 3-4x/day; doesnt alter progression of disease; dyskinesa more common

Selegiline**

→ inhib. MAOb (↓ striatal metab of DA); MAOa at ↑ doses;

may ↓ progession (↓ h2o2);
amphetamine like metabolite (insomnia)

Rasagiline

→ irreversibe MAO-B inhib; no amphetamine like metabolites, no tyramine restriction

Bromocriptine**

Dopamine Agonist:
→ D2 agonist; 
-effectiveness does not ↓
-↓ prolactin; 
-GI SE, postural hypoTN, arrythmias (same as l-dopa)

-vasospasm SE (erythromelagia, pulmonary fibrosis)

Pergolide

Dopamine Agonist:

→ D1 & D2 agonist; sudden sleep

Pramipexole**

Dopamine Agonist:
→ NO erythromelalgia, vasospasm, fibrosis;
-can cause sudden sleep; well tolerated
-on/off less likely

Ropinirole**

Dopamine Agonist:
→ treatment for RLS
→ NO erythromelalgia, vasospasm, fibrosis; can cause sudden sleep; well tolerated, on/off less likely

Amantadine

→ antiviral for flu; ↑ release of DA (less potent than L-dopa); toxic psycosis & convulsions (OD) spotting of skin & edema; caution w/ history of seizure or CHF

Benztropine**

→ ↓ effects of ACh to balance loss of DA;

-improves rigidity & tremor (not bradykinesia)

Donepezil**
Rivastigmine
Galantamine

Cholinesterase Inhibitors
↓ breakdown of ACh in synaptic cleft
-may slow course of disease
-GI side-effects, ↑ stomach acid & salivation

Memantine

→ NMDA antagonist; ↓ extra-synaptic NMDA glutamate toxicity;

↑ SE of l-dopa & DA agonists;

-SE agitation, urinary incontinence, UTI,

Flumazenil**

→ competes w/ benzo for receptor;
-IV admin slowly in series to ↓ risk of seizures (DoA 30 min)

reverse effect of: Midazolam, zolpidem, zaleplon, eszopiclone
can cause seizure in pts w/ barb or TCA overdose; DO NOT use if signs of seizures

Zolpidem**

→ bind BZ1 subtype; 2hr half-life

-minor effect on REM

Zaleplon

→ bind BZ1 subtype; 1hr half-life

-minor effect on REM

Eszopiclone

→ less selective (more like benzo) 6hr half-life; long term treatment of insomnia
-minor effect on REM

Ramelteon**

→ MT1 & MT2; shortens delay to sleep onset;
-extensive 1st pass metab. (caution w/ liver diease, dont use w/ severe liver problems)

SIDE EFFECTS

↑ prolactin & ↓ testosterone
headache, rash

Buspirone**

→ partial agonist 5-HT1; relieves anxiety w/o sedation; 2 wks to take affect

↓ serotonin release
↑ noradrenergic & DAnergic pathways
no effect on bento or GABA receptors
-LOW addiction potential
-good for ADDICTS & ELDERLY
no sedation**
doesnt affect memory**

+ MAOI → severe HTN or serotonin syndrome

Chloral hydrate**

→ converted to trichloroethanol, binds GABAa

acts similar to barbiturates (low safety)
-respiratory and vasomotor depression
-tolerance and dependance
-liver danage & fatal intoxication

-pediatric dental procedures

Diphenhydramine**

→ blocks H1 receptor, anti-ACh; good choice for insomnia in addicts to alcohol or benzo

Naltrexone**

→ blocks ability of alcohol to simulate reward pathway (B-endorphin)
↓ craving (↓ rate of relapse by 50%); nausea, large dose → liver damage, opioid wont work

Acamprosate

→ structural analogue of GABA; restores normal balance of GABA/Glutamte transmission
(NO LIVER TOXICITY → DOC for pts w/ liver disease)

Disulfiram**

→ blocks ALDEHYDE dehydrogenase; long duration; inhib p450

lots of side-effects and drug interactions; not recommended

Drugs most likely to cause Steve Johnson syndrome

HLA-B*1502

phenytoin, fosphenytoin
phenobarbital, primidone
lamotrigene
ethosuximide
valproic acid

Phenobarbital

→ long lasting; anticonvulsant
↑ duration of GABA action

Contraindicated in:
-porphyria (↑ synthesis)

Thiopental

ultra-short acting; induction of anesthesia

↑ duration of GABA action

Benzodiazepines duration of action

Long lasting:

Diazepam
Chlordiazepoxide
flurazepam
chlorazepate (inactive)

Intermediate:

oxazepam
lorazepam

short acting:

alprazolam
triazolam

very short acting:
-midazolam

Diazepam**

muscle relax, anticonvulsant (status epilepticus), alcohol/barb withdrawl

-cimetidine ↓ metabolism

-long lasting
↑ actions of GABA

Contraindicated in:

pregnancy (category D)
children (elderly confusion)
sleep apnea
w/ alcohol use