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106 Cards in this Set
- Front
- Back
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What are the typical antipsychotics?
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Haloperidol + "azine"s
work by inhibiting D2 dopamine receptors |
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What are the low-potency typical psychotics?
What type of side-effects? |
Thioridazine, chlorpromazine
-non-neuro side-effects -arise from blocking muscarinic (dry mouth, constipation); alpha (hypotension); and histamine (sedation) receptors |
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Explain the evolution of Extrapyramidal (EPS) side-effects
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4h acute dystonia (spasm, stiffness)
4d akinesia (parkinsonian) 4wk akathasia (restlessness) 4mo tardive diskinesia (oral-facial movements-->irreversible) |
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What is NMS? tx?
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F:ever
E:ncephalopathy V:itals unstable E:levated enzymes R:igidity of muscles Dantrolene (prevents release of Ca2+ from SR) |
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Malignant Hyperthermia? tx?
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concomitant use of inhalation anesthetics and succinylcholine
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Atypical Antipsychotics
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Clozapine
Olanzapine Risperidone Aripipazole Quietapine Ziprasidone -work by blocking 5-HT2, alpha, and H1 receptors |
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What are atypical antipsychotics used for
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+ and neg symtpoms of schizophrenia
-olanzapine is also used for OCD, anxiety, depression, mania, and Tourette's |
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Side-effects of clozapine
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agranulocytosis
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Lithium side-effects
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M:ovement (tremor)
N:Nephrogenic DI O:hypOthyroidism P:regnancy probs |
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Buspirone MOA and use?
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stimulates 5-HT1A receptors, used for generalized anxiety disorders, no sadation or addicition, no interaction with alchohol
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What class of drug is Imipramine? Clomipramine? Nortriptyline? Doxepin?
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TCA
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WHat TCA is used to treat bedwetting?
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Imipramine
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How do TCAs work?
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block reuptake of NE
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What toxicity of TCAs?
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Convulsions
Coma Cardiotoxicity (arythmias) resp Depression Hyperpyrexia |
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Which TCA should be used in elderly?
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nortryptyline because of confusion and hallucinations (anticholinergic side-effects)
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What is treatment for CV toxicity of TCAs
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NaHCO3
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What is the least sedating TCA?
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despiramine
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Name some SSRIs
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fluoxetine, sertraline, citalopram, paroxetine
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Uses of SSRIs
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Depression, OCD
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Toxicities of SSRIs
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GI upset, anorgasmia
"Serotonin syndrome" with MAOs -hyperthermia -muscle rigidity -CV collapse -flushing -diarreah |
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How long do SSRIs take to work?
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2-3wks
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What is Buproprion used for and how work?
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Increased dopamine and NE
-smoking cessation and depression |
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Side effects of Buproprion
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adrenergic stimulating effects,
headache, seizure in bulemics, no sexual side effects |
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venlafaxine uses, toxicity, and MOA
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depression and generalized anxiety disorder.
Inhibits NE and serotonin reuptake Tox: incr BP sedation, nausea |
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Difference between Duloxetine and venlafaxine
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more effect on NE with duloxetine, and also used in peripheral neuropaty
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What is Mirtazapine and how work?
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alpha2 antagonist (incr NE and serotoinin release) also blocks 5-HT2 and 5-HT3 receptors
use for depression |
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How does Maprotiline work? use?
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Blocks NE reuptake
-for depression -can lead to sedation, and orthostatic hypotension |
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How does traxodone work? side-effects?
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inhibits serotonin reuptake
used for insomnia, as high doses would be needed for antidepressant effects -nausea, priapism, post. hypo |
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name two MAO inhibs?
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phenelzine, trancyclopramine
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Uses for MAO inhibs?
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atypical depression, anxiety, hypochondriasis
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toxicity of MAOs
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hypertensive crisis with ingestion of tyramine and beta-agonists. contraindicated with SSRIs and meperidine-->SS
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What is the treatment of choice for depression with insomnia and how does this drug work?
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Mirtazapine: alpha2 antagonist-->incr NE and 5-HT2/3 antagonist
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OCD treatment?
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SSRIs
Clomipramine |
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TX for PTSD?
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SSRIs
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Tx for Bipolar?
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Lithium, Valproic Acid, Carbamazepine
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What is tx for Anxiety?
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Bensodiaz, SSRIs, Buspirone
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Diff between tx for atypical and typical depression?
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Typical: SSRIs, NSRIs, TCAs
Atypical: MAO inhibs, SSRIs |
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ADHD tx
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Methyphenidate
Amphetamines |
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Tx for Tourette's
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Haloperidol
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Dantrolene
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tx fo neuroleptic malignant syndrome (toxicity of antipsychotics); also for succinylcholine and inhaled anaesthetic-induced malignant hyperthermia
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Selegiline
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MAO-B inhibitor: increases availability of dopamine
used with L-dopa for Parkinson's |
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When is sumatriptan contraindicated and why?
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causes coronary vasospasm (contraindicated in patients with CAD or Printzmetal's angina)
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What is sumatriptan used to treat and how does it work?
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5-HT1B/1D agonist.
causes vasoconstriction and inhibition of trigeminal activation, vasoactive peptide release Half-life<2hrs used for acute migraine and cluster headaches |
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What is Memantine and how does it work?
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NDMA receptor antagonist used to help prevent excitotoxicity in Alzheimer's
-can cause diziness, confusion, hallucinations |
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Donepezil
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Ach-esterase Inhibitor
used for Alzheimer's |
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Why is carbadopa given with Levadopa to Parkinson's patients?
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carbidopa is a peripheral carboxylase inhibitor and increases bioavailability in the brain while reducing peripheral side-effects
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WHy is L-dopa given instead of dopamine to Parkinson's patients?
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L-dopa can cross BBB
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How does Amantadine work and what besides parkinson's is it used to treat?
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increases dopamine release.
also used to treat InfluA and rubella |
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How does Bromocriptine work? what are similar drugs?
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Pramipexole, ropinerole
works as an ergot alkaloid/dopamine agonist |
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What is benztropine used in?
what does it fix an what can it not fix |
Antimuscarinic-->improved tremor and rigidity.
little action against bradykinesia |
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How are essential or familial tremors treated?
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beta-blocker
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What are entacapone and tolcapone?
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COMt inhibitors
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What are neuromuscular blocking drugs used for?
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muscle paralysis in surgery and mechanical ventilation
-specific for muscle nicotinic receptors |
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What is Phase I of a depolarizing blockade and what is the effect of chonlinesterase inhibitors?
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Prolonged depolarization with no antidote.
the block is potentiated by cholinesterase inhibitors -no antidote |
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What is Phase II of a depolarizing blockade and what is the effect of cholinesterase inhibitors?
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repolarized but blocked-->antidote is cholinesterase inhibitor (neostigmine)
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Name some Nondepolarizing neuromuscular blockers
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Tubocurarine
Atracurium Mivacurium Pancuronium Vecuronium Rocuronium compete with Ach for revceptors -reversed by Cholinesterase inhibitors (neostigmine, edrophonium, and other cholinesterase inhibs) |
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What kind of drug is succinylcholine and what are some adverse effects?
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Depolarizing Neuromuscular blocker
can cause hyperkalemia and hypercalcemia |
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What are some ester local anaesthetics?
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Procaine
Cocaine Tertracaine |
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name the AMide anasthetics
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lIdocaIne, mepIvacaIne, bupIvacaIne
-two "I's" |
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Side-effect of bupivicaine
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Severe cardiotoxicity, CNS excitiation
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If someone is allergic to esters, what class of drug should be used?
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AMIDES-liocaine, mepivacaine, bupivacaine
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How do local anaesthetics work?
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preferentially bind to and inactivate active nA+ CHANNELS-->most effective in rapidly-firing neurons
-tertiary amines can penetrate BBB in uncharged forma nd then bind to ion channels in charged form |
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how do Arylcyclohexylamines work?
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ketamine is a PCP analog that act as dissociative anaesthetics-->bind to NMDA receptor
--.cause increased cerebral blood flow and disorientaition as well as CV stim. |
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What is the most common benzodiaz used for endoscopy and what is it used with?
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Midazolam in conjunction with gaseuous anaesthetics and narcotics
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How treat a benzo overdose?
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FLUMENAZIL
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What is methoxyflourane?
Name 5 other similar drugs. |
Inhaled Anaesthetic:
halothane, enflurane, isoflurane, sevoflurane, N2O |
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What are the effects of enflurane?
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Myocard Depression, Respiratory depression, nausea/emesis, increased cerebral BF
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What is the toxicity of halothane?
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hepatotoxicity
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Toxicity of methoxyflurane?
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nephrotoxicity
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Toxicity of N2O?
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trapped gas expansion
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How do drugs get into CNS?
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lipid-soluble or active transport
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If a drug has a low blood solubility what will this lead to?
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Rapid Induction and recovery times
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If a drug has a high solubility in lipids, what will this lead to?
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Increased potency and decreased MAC
potency = 1/MAC |
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What is MAC?
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The minimal alveolar concentration at which 50% of pop is anesthetized.
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What is the induction time and potency of N2O?
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N2O has a high induction and low potency because it is poorly soluble in blood AND lipids
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What is the induction time and potency of halothane?
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halothane has high solubility in blood and lipids so it has a slow induction/recovery time and a high potency
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How do benzodiazepines work
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facilitate GABAa action by increasing frequency of Cl- channel opening, also decr REM sleep
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SHort-Active benzos?
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T:riazolam
O:xezepam M:idazolam -these have the highest addictive potential. |
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When are benzos used?
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Anxiety
Spasticity Status Epilepticus (lorazepam and diazepam) Detox (DTs) night terrors sleepwalking |
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Toxicity of Benzos?
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dependance, additive CNS depressive effects with alcohol
less risks than barbiturates |
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How do Barbiturates work?
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barbiDURATEs increase duration of Cl- channel opening at GABA receptors
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Name some barbiturates and tell their uses
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THiopental, Phenobarbital, pentobarbital, secobarbital
-used for sedation of anxiety, insomnia -thiopental is also used for anaesthesia induction |
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toxicity of Barbiturates
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dependence, additive CNS depression with alcohol, resp or CV depression-->death, CYP-450 inducers
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How does Phenytoin work?
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blockade of Na+ channels; inhibition of glutamate release from presynaptic excitatory neuron
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What is phenytoin used for and toxicity?
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Tonic-Clonic seizures
Class IB antiarrythmic tox: nystagmus, ataxia, SLE-like syndrome, CYP-450 inducer gingival hyperplasia peripheral neuropathy megaloblastic anemia (secondary to decr folate abs) hirsutism teratogenic (fetal hydantoin syndrome) |
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What are first line tx for tonic-clonic seizure?
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phenytoin, carbemazepine, valproic acid
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How does Lamotrigline work?
Side-effects? |
Blocks voltage-gated Na+ channels.
Tox: Stevens-Johnson Syndrome |
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What is first line tx for abscence seizures?
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Ethosuxamide
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MOA and Side-effects of ethosuxamide?
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blocks thalamic T-type ca2+ channels
F:atigue G:I H:eadache and Stevens-Johnson |
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Valproic acid MOA and toxicity?
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increase Na+ channel inactivation;
increased GABA conc. Tox: GI upset rare, fatal hepatotoxicity SPINA BIFIDA IN FETUS (contraindicated in pregnancy) tremor weight gain |
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How does Gabapentin work and side-effects
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Increased GABA release
used in simple, complex, t-c and peripheral neuropathy -side-effects; sedation and ataxia |
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What are two first line agents for status epilepticus?
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Lorazepam (diazepam) and phenytoin
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What is first line treatment for seizures of preecclampsia?
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MgSO4 and benzos
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How does Topiramate work and side effects.
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-blocks Na+ channels and increased GABA action
tox: sedation, mental dullness, kidney stones, weight loss. |
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What is carbemazepine used to treat and what are its side effects?
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increases Na+ channel inactivation
used for simple, complex and 1st line for T-C and TRIGEMINAL NEURALGIA toxicities: diploplia, ataxia, agranulocytosis, aplastic anemia, liver tox, teratogenesis, CYP-450 inducer |
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What is tramadol?
useage toxicity |
-weak opioid agonist-
-inhibits serotonin and NE reuptake "TRAM-it'ALL" used clinically for : chronic piain is addictive, resp depression, decreased seizure threshold |
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Butorphanol
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partial opioid MU receptor agonis, agonist at kappa receptors
used to treat pain; less resp depression than full agonists -causes withdrawal of full opioid agonists |
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How do opioid agonists work?
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open K+ channels, close ca2+ channels-->decr synaptic transmission
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Tolerance to what does not develop when on opioids?
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constipation and miosis
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What diuretic is useful in Glaucoma?
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Acetozolamide-->decreased carbonic anyhdrase activity-->decreased HCO3- production-->decreased aqueous humor production
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What are two alpha agonists used in treatment of glaucoma?
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epinephrine causes decr aq. humor production due to vasoconstriction (do not use in closed-angle glaucoma)
brimonidine causes decre aqueous humor synth |
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WHat is broimonidine used for?
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glaucoma (alpha-agonist)
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What beta-blockers are used in glaucoma tx?
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timolol, betaxolol, carteolol
-decreased aqueous humor secretion |
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What is Lantaprost used for?
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(PGF2alpha) used to increase outflow of aqueous humor
may darken iris color (browning) |
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What is pilocarpine used for?
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Pilocarpine (emergencies) increased the outflow of aqueous humor; it contracts the ciliray muscle to open the trabecular network-->open canal of Schlemm
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What are carbachol, echothiophate, and physostigmine used for?
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cholinomimetics used for tx of gluacoma
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