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197 Cards in this Set
- Front
- Back
1.Triazolam, Oxazepam and Midazolam are what types of drugs?
2. What is the mechanism of their drug family? |
1.Short acting Benzodiazepine
2. Facilitate GABAa action by increasing the frequency of Cl- channel opening |
|
1. Thiopental and Secobarbital are what types of drugs?
|
1. Barbiturates
|
|
1.Chlordiazepoxide is what type of drug?
2. How would you treat an overdose of this family of drugs? |
1.Benzodiazepine
2. Flumazenil (a competitive antagonist at GABA receptor) |
|
1.Chlorpromazine and Fluhenazine are what types of drugs?
2. Tx for what? |
1.Typical Antipsychotics
2. Schizophrenia and Psychosis |
|
What is Buspirone?
Tx? Mechanism? Side effect? |
1.Partial agonist: Non-benzodiazepine 2.Chronic generalized anxiety
3.Relieves anxiety without sedation, hypnosis or addiction) 4. Tachycardia or gastrointestinal anxiety. |
|
How do you treat arrhythmias due to Hyperthroidism?
Possible mechanism of this arrhythmia? |
1. Beta-blocker
2. Hyperthroidism upregulates B-adenergic receptors |
|
Nitropusside toxicity (nitrate side effect)?
|
1. Can produce thiocynate (can starve cells to death because of it can replace oxygen as the electron acceptor in respiration oxidation)
|
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Define Sedation?
|
Decrease anxiety, motor activity and mental acuity
|
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Define Hypnosis?
|
Drowsiness and increased tendency to sleep
|
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Are benzodiazepine are they hypnotic, sedative or anxiolytic(or subset of sedative: anxiolytic)?
|
Various benzodiazepine have varying properties of all three
Hypnotic, sedative or anxiolytic. Hypnotic and anxiolytic are popular xteristics |
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What is another name for Triazolam - a short acting Benzodiazepine?
2.what about Diazepam (long acting)? 3. What about Alprazolam (intermediate)? |
1. Triazolam - Halcion
2. Diazepam - Valium 3. Alprazolam - Xanax |
|
Another name for Zolpiden?
Tx for? |
1. Zolpiden - Ambien
2. Short-term treatment of Anxiety |
|
What is the drug of choice to Tx of anxiety and isomnia?
what is else can Benzodiazpine tx? Mechanism? |
1.Benzodiazepine
Anxiety (sedative) Isomnia (hypnotic effect) 2. Seizures, Spasms (muscle relaxation) 3. Increase the seizure threshold |
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What benzodiazepine is the drug of choice for Tx of Panic disorders and Agoraphobia?
|
Alprazolam (Xanax): intermediate
|
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Aside from insomina and anxiety - what is else can Benzodiazpine tx?
Mechanism? |
1. Seizures, Spasms (muscle relaxation)
2. Increase the seizure threshold |
|
Name the benzodiazepines used for Seizures?
Type of seizure? Name the preferred Benzodiazepine for the pediatric population? |
1.Diazepam - IV infusion
2. Status Epilepticus and drug and toxin induced seizure 3. Lorazepam |
|
Possible effects of Benzodiazepine in
Cardiovascular? Combo with another depressor(e.gETOH)? Fetus? |
1. Decrease BP and heart rate
2. CNS depression 3. Benzodiazepine accumulate in the fetus |
|
what is the mechanism of action of L-dopa/carbidopa
|
increase dopamine level in brain
|
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how is L-dopa different from dopamine
|
L-dopa can cross the blood-brain barrier, dopamine cannot
|
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what happens to L-dopa after it crosses the BBB
|
converted to dopamine by dopa decarboxylase
|
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what is the function of carbidopa
|
peripheral decarboxylase inhibitor
|
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what are the side effects of L-dopa.carbidopa treatment
|
arrhythmias, dyskinesias
|
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1.why do patients taking L-dopa get arrhythmias?
2.dyskinesias? |
1.peripheral effects of dopamine
2.excess dopamine stimulation in CNS |
|
specifically, which drugs are used to treat Parkinson's
|
Bromocriptine, Amantadine, Levodopa, Selegiline, Antimuscarinics (BALSA)
|
|
which dopamine agosts are used to treat Parkinson's
|
L-dopa/carbidopa, bromocriptine, pramipexole, ropinirole, amantadine
|
|
what is the action of bromocriptine in Parkinson's
|
ergot alkaloid, partial dopamine agonist
|
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what is the action of amantadine in Parkinson's
|
enhances dopamine release
|
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what MAOI is used to treat Parkinson's?
Describe its site of action? |
1.selegiline
2.selective MAO type B inhibitor |
|
1.what antimuscarinic is used to treat Parkinson's?
2. What Si/Sx does it treat? |
1.benztropine
2.improves tremor, rigidity, little effect on bradykinesia |
|
what is the effect of benztropine in Parkinson's
|
improves tremor, rigidity, little effect on bradykinesia
|
|
1.what is sumatriptan used for?
2.What type of drug is it? 3. What is it's T1/2? |
1.acute migraine, cluster headache attacks
2. 5-HT1D agonist 3. less than 2hours |
|
1.what are the side effects of sumatriptan (tx for migraine)?
2.Mechanism? 3.What are the contraindication? |
1.Chest discomfort, mild tingling
2.Vasoconstrict in the brain 3. Patients with CAD or Prinzmetal's angina |
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which drugs are used for simple and complex partial seizures
|
phenytoin, carbamazapine, lamotrigine, gabapentin, topiramate, phenobarbital
|
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what types of seizures is phenytoin indicated for
|
simple and complex partial, tonic-clonic, status epilepticus
|
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1. Name four drugs that can be used to treat all three seizures
simple and complex partial, tonic-clonic |
1.Phenytoin
2.Carbamazepine 3.Lamotrigne 4.Gabapentin 5.Phenobarbital |
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what are lamotrigine and topiramate used to treat?
|
1.simple and complex partial, tonic-clonic
Topiramate not used for tonic clonic |
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what types of seizures is gabapentin indicated for
|
simple and complex partial, tonic-clonic
|
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what types of seizures is topiramate indicated for
|
simple and complex partial
|
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what types of seizures is phenobarbital indicated for
|
simple and complex partial, tonic-clonic
|
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what drugs can be used for tonic-clonic seizures
|
phenytoin, carbamazapine, lamotrigine, gabapentin, phenobarbital, valproate
|
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what drugs can be used for absence seizures
|
valproate, ethosuximide
|
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what drugs can be used for status epilepticus
|
phenytoin, benzodiazapines (diazepam, lorazepam)
|
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what types of seizure is valproate indicated for
|
tonic-clonic, absence
|
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what types of seizure is ethosuximide inidcated for
|
absence
|
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what type of seizure are benzodiazepines indicated for
|
status epilepticus
|
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other than anti-seizure, what else is phenytoin used for
|
class 1B anti-arrhythmic
|
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how should a patient taking carbamazepine be followed
|
monitor LFT's weekly
|
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which seizure drugs have adjunct use
|
gabapentin, topiramate
|
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which seizure drug is safest in pregnant women
|
phenobarbital
|
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which seizure drug is used in Crigler-Najjar II
|
phenobarbital
|
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what are the side effects of phenytoin
|
nystagmus, diplopia, ataxia, sedation, ginigival hyperplasia, hirsutism, anemias, teratogenic
|
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what are the side effects of valproate
|
GI distress, rare by fatal hepatotoxicity, neural tube defects (spina bifida)
|
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what are the side effects of lamotrigine
|
life-threatening rash, Stevens-Johnson syndrome
|
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what are the side effects of gabapentin
|
sedation, movement disorders
|
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what are the side effects of topiramate
|
sedation, mental dulling, kidney stones, weight loss
|
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which anti-epileptic drug is teratogenic
|
phenytoin
|
|
which anti-epileptic drug can cause dependence
|
benzodiazepines, phenobarbital
|
|
which anti-epileptic drug can cause neural tube defects
|
valproate
|
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which anti-epileptic drugs can cause GI distress
|
valproate, ethosuximide
|
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it is necessary to check LFT's with which anti-epileptic drugs
|
carbamazepine, valproate
|
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which anti-epileptic drugs cause CYP induction
|
phenobarbital, carbamazepine
|
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which anti-epileptic drugs can cause blood problems
|
carbamazepine, phenytoin
|
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which anti-epileptic drugs can cause Stevens-Johnson syndrome
|
lamotrigine, ethosuximide
|
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which anti-epileptic drugs can cause diplopia
|
carbamazepine, phenytoin
|
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what is the mechanism of phenytoin action
|
use-dependent blockade of Na+ channels
|
|
what is the clinical application of phenytoin
|
grand mal seizures
|
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what are the toxicities of phenytoin
|
nystagmus, ataxia, diplopia, lethargy, SLE - drug induced(HIPP)
|
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what are the chronic toxicities of phenytoin
|
gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia, malignant hyperthermia (rare)
|
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should pregnant women take phenytoin
|
NO -- teratogenic
|
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Name the drug used in epilespy treatment that can cause megaloblastic anemia?
|
Phenytonin
|
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name 4 barbiturates
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phenobarbital, pentobarbital, thiopental, secobarbital
|
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what is the mechanism of barbiturate action
|
increase duration of Cl channel opening --> decreased neuron firing --> facilitate GABA-A action
|
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how do barbiturates facilitate GABA-A action and can act as GABA agonist -
Therefore at high doses may cause CNS depression which is less likely with benzodiazapine |
increase duration of Cl channel opening which decreases neuron firing (Barbidurate increases duration
|
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what is the clinical application of barbiturates
|
sedative for anxiety, seizures, insomnia, anesthesia induction (thiopental)
|
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which barbiturate is used for anesthesia induction
|
thiopental
|
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what are the side effects of barbiturates
|
1.dependence,
2.Additive CNS depression effects with alcohol, 3.respiratory or CV depression (death), 4. Induces P-450: drug interactions due to CYP induction |
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what should you find out before giving a patient barbiturates
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what other medications they take, because of CYP induction and many drug interactions
|
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what happens if you give barbiturates to a patient in alcohol-induced coma or DT's
|
they might DIE!! Because of additive effect of barbiturates and alcohol --> respiratory depression
|
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when are barbiturates contra-indicated
|
porphyria
|
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name a bunch of benzodiazepines
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diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide (all have ZZZ in them)
|
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what is the mechanism of benzodiazepines
|
increase frequency of Cl channel opening --> facilitate GABA-A action (Frenzodiazepines increase frequency)
|
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which GABA receptors are facilitated by barbiturates and bezodiazepines
|
GABA-A
|
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what are the clinical applications of benzodiazepines
|
anxiety, spasticity, status epilepticus (diazepam), detoxification (alcohol withdrawal, DT's)
|
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which benzodiazepine can be used for status epilepticus
|
diazepam
|
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what drugs can be used to treat alcohol withdrawal
|
benzodiazepines
|
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which benzodiazepines are short-acting
|
TOM thumb: Triazolam, Oxazepam, Midazolam
|
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how are benzos better than barbiturates
|
less respiratory depression and coma risk
|
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how do you treat benzo overdose?
Mechanism of the drug? |
1.flumazenil
2.Competitive GABA antagonist |
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are barbiturates or benzodiazepines used for alcohol withdrawal
|
benzodiazepines
|
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what is another name for antipsychotics
|
neuroleptics
|
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name 4 antipsychotic drugs
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thioridazine, haloperidol, fluphenazine, chlorpromazine
|
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how do you keep benzos straight from antipsychotics
|
Benzos help 3rd year Jon Kazam be less anxious around patients: Shazam Kazam! Without antipsychotics patients talk like a crazy 'zine (well, not perfect, but I'm working on it)
|
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what is the mechanism of most antipsychotics
|
block dopamine D2 receptors
|
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what is the clinical application of antipsychotics
|
schizophrenia, psychosis
|
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what are the side effects of antipsychotics
|
extrapyramidal side effects (EPS), sedation, endocrine, muscarinic blockade, alpha blockade, histamine blockade
|
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what is a long-term effect of antipsychotic use
|
tardive dyskinesia
|
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what is neuroleptic malignant syndrome?
how do you treat neuroleptic malignant syndrome? |
1.Side effect of antipsychotics; rigidity,
autonomic instability, hyperpyrexia 2.dantrolene, dopamine agonists |
|
what is tardive dyskinesia?
Reversible or irreversible? Cause of Tardive dyskinesia? |
1. side effect of neuroleptics; stereotypic oral-facial movements, may be due to dopamine receptor sensitization
2. Irreversible 3. Neuroleptics, or side effect of parkinson drugs |
|
what is the "rule of 4" with EPS side effects from antipsychotic drugs
|
evolution of EPS side effects:
4 hours -- acute dystonia, 4 days -- akinesia, 4 weeks -- akasthesia, 4 months -- tardvie dyskinesia |
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is tardvie dyskinesia reversible
|
often irreversible
|
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what is fluphenazine? used for
Other similar drugs are Thioridazine. Name the rest? |
1.schizophrenia, psychosis
2. Chlorpromazine, Haloperidol |
|
name 3 atypical antipsychotics?
what is the mechanism of atypical antipsychotics? Tx of? |
A.Clozapine,
B.Olanzapine- great for OCD,anxiety,depression C. Risperidone 2.block 5-HT2 and dopamine receptors 3. Schizophrenia - useful for the Positive and negative Si/Sx |
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what type of antipsychotic is clozapine
|
atypical
|
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what type of antipsychotic is olanzapine
|
atypical
|
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what type of antipsychotic is risperidone
|
atypical
|
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how are atypical antipsychotics different from classic ones
|
atypicals treat positive and negative symptoms of schizophrenia, fewer extrapyramidal and anticholinergic side effects than classic antipsychotics
|
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which antipsychotics should be used for fewer side effects
|
atypical ones -- clozapine, olanzapine, risperidone
|
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what is a potential toxicity of clozapine?
What is clozapine? |
1.agranulocytosis
2. Atypical antipsychotic |
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what test must be done weekly on patients taking clozapine
|
WBC count because of potential agranulocytosis
|
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what is the mechanism of action of lithium
|
unknown; may be related to inhibition of phosphoinositol cascade
|
|
what is the clinical application of lithium?
How does it work |
1.mood stabilizer for bipolar disorder
2.Prevents relapse and acute manic episodes |
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how does lithium help people with bipolar disorder
|
prevents relapse and acute manic episodes
|
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what are the side effects of lithium
|
tremor, hypothyroidism, polyuria, teratogenic
|
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is it OK for women taking lithium to get pregnant
|
NO -- teratogenic
|
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what does lithium cause polyuria
|
ADH antagonist --> nephrogenic diabetes insipidus
|
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What do the following drugs inhibit: 1. MAO inhibitors, 2. Desipramine/maprotilline, 3. Mirtazapine and 4. Fluoxetine/trazodone?
A. Site of action for these drugs? |
1. MAO 2. NE reuptake 3. Alpha 2-R 4. 5HT reuptake
A.Pre-synaptic |
|
List the Tricyclic Antidepressants
|
pg 311 Imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin
|
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What are the three C's of their toxicity?
|
Convulsions, Coma, Cardiotoxicity (arrythmias). Also respiratory depression, hypyrexia.
|
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How about toxicity in the eldery?
|
confusion and hallucinations due to anticholinergic SE
|
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What is the mechanism of TCA?
|
block reuptake of NE and 5HT
|
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What is the clinical uses of TCAs?
|
Endogenous depresion. Bed wetting - imipramine. OCD- clomipramine.
|
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How are tertiary TCA's different than secondary in terms of side effects?
|
Amitriptyline (tertiary) has more anti-cholinergic effects than do secondary (nortriptyline). Desipramine is the least sedating.
|
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what are the SE of TCAs?
|
sedation, alpha blocking effects, atropine-like anti cholinergic side effects (tachycardia, urinary retention)
|
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Fluoxetine, sertraline, paroxetine, citalopram are what class of drugs?
|
pg 311 SSRI's for endogenous depression
|
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How long does it take an anti-depressant to have an effect?
|
2-3weeks
|
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How SSRI toxicity differ from TCA's and what are they?
|
Fewer than TCA's. CNS stimulation - anxiety, insomnia, tremor, anorexia, nausea, and vomiting.
|
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What toxicity happens with SSRI's and MAO inhibitors given together?
|
Seratonin Syndrome! Hyperthermia, muscle rigidity, cardiovascular collapse
|
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What are heterocyclics?
|
2nd and 3rd generation antidepressants with varied and mixed mechanisms of action. Used major depression.
|
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Examples of heterocyclics?
|
trazodone, buproprion, venlafaxine, mirtazapine, maprotiline
|
|
1.Which heterocyclic is used for smoking cessation?
2.What is its toxicities? |
1.Buproprion. Mechanism not known. 2.Stimulant effects, dry mouth, aggrevation of pyschosis
Used for Major depression Tx |
|
Which of the Heterocyclics is used in GAD?
Mechanism? Toxic effects? |
1.Venlafaxine -
2.inhibits 5HT and DA reuptake. 3.Toxicity - stimulant effects |
|
which is the only heterocyclic blocks NE reuptake?
What heterocyclic increases the release of NE and serotonine and potent 5-HT2 receptor antagonist? |
1.maprotiline
2. Mirtazapine |
|
What is trazodone and it' SE?
|
primarily inhibits seratonin reuptake. Toxicity - sedation, nausea, priapism, postural hypotension
|
|
Give 2 examples of MAO?
Mechanism and Clinical Uses? |
1.Phenelzine and Tranylcypromine
2.Non selevtive MAO inhibition. 3.Atypical antidepressant, anxiety, hypochondriasis |
|
What is the toxicity with tyramine ingestion (in foods) and meperidine when using MAO?
|
1.Hypertensive crisis
non-selective Phenelzine and Tranylcypromine selective - selegiline |
|
Apart from hypertensive crisis with wine and cheese- What drugs are MAO contraindicated for?
|
Contraindicated with SSRI's or B-agonists
Other toxicities: CNS stimulation |
|
What is the mechanims of selgiline (deprenyl)?
What is the side effect when used with L-dopa for the treatment of Parkinson? |
1.Selectively inhibits MAO-B, increasing DA
2.May enhance the adverse effects of L-Dopa (such as dyskinesia, prolactin reduction) |
|
What is the significance of drugs with decreased solubility in blood?
|
rapid induction and recovery times . Ie. N20
(may be put under pressure to deliver it in the lungs) |
|
What is the significance of drugs with increased solubility in blood?
|
increased potency = I/ MAC. Ie. Halothane
|
|
list the Inhaled Anesthetics? Which is the most potent?
|
halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
|
|
What are the effects inhaled anesthetics? (not toxicity effects)
Some inhaled A.: Enflurane,sevoflurane |
myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow
|
|
List the Tricyclic Antidepressants
|
pg 311 Imipramine, amitriptyline, desipramine, nortriptyline, clomipramine, doxepin
|
|
What are the three C's of their toxicity of Tricyclic Antidepressants?
|
Convulsions, Coma, Cardiotoxicity (arrythmias). Also respiratory depression, hypyrexia.
|
|
How about toxicity in the eldery?
|
confusion and hallucinations due to anticholinergic SE
|
|
What is the mechanism of TCA?
|
block reuptake of NE and 5HT
|
|
What is the clinical uses of TCAs?
|
Endogenous depresion. Bed wetting - imipramine. OCD- clomipramine.
|
|
How are tertiary TCA's different than secondary in terms of side effects?
|
Amitriptyline (tertiary) has more anti-cholinergic effects than do secondary (nortriptyline). Desipramine is the least sedating.
|
|
what are the SE of TCAs?
|
sedation, alpha blocking effects, atropine-like anti cholinergic side effects (tachycardia, urinary retention)
|
|
Fluoxetine, sertraline, paroxetine, citalopram are what class of drugs?
|
pg 311 SSRI's for endogenous depression
|
|
How long does it take an anti-depressant to have an effect?
|
2-3weeks
|
|
How does the toxicity of SSRI's differ fromTCA's and what are they?
|
Fewer than TCA's. CNS stimulation - anxiety, insomnia, tremor, anorexia, nausea, and vomiting.
|
|
What toxicity happens with SSRI's and MAO inhibitors given together?
|
Seratonin Syndrome! Hyperthermia, muscle rigidity, cardiovascular collapse
|
|
What are heterocyclics?
|
pg 312 2nd and 3rd generation antidepressants with varied and mixed mechanisms of action. Used major depression.
|
|
Examples of heterocyclics?
|
trazodone, buproprion, venlafaxine, mirtazapine, maprotiline
|
|
1.Which Heterocyclic is used for smoking cessation?
2. The Toxic effect of the drug? |
Buproprion. Mechanism not known. Toxicity - stimulant effects, dry mouth, aggrevation of pyschosis
|
|
Which Heterocyclic is used in Generalized Anxiety Disorder?
Mechanism? what are its Toxicity? |
1.Venlafaxine -
2.inhibits 5HT and DA reuptake. 3.Toxicity - stimulant effects |
|
which heterocyclic blocks NE reuptake?
|
maprotiline
|
|
Which heterocyclic increases release of NE and 5HT via alpha 2 antagonism?
|
1. Mirtazapine. Also potent 5HT-R antagonist.
2. Toxicity - sedation, increase serum cholesterol, increase appetite |
|
What is trazodone? Mechanism? and it' SE?
|
1. Heterocyclic (main job of this family is major depressive disorders)
2.Inhibits seratonin reuptake. 3.Sedation, nausea, priapism, postural hypotension |
|
Give 2 examples of MAO
|
Phenelzine
Tranylcypromine |
|
What are phenelzine and Tranylcypromine?
Mechanism and Clinical Uses? Contraindicated with what? |
1.non selevtive MAO inhibition.
2. Atypical antidepressant(with psychotic and phobic elements), anxiety, hypochondriasis 3. SSRI and B-agonist |
|
What is the toxicity with tyramine ingestion (in foods) and meperidine?
|
Hypertensive crisis
|
|
Other toxicities of MAO inhibitors aside from tyramine ingestion? Contraindication?
|
1.CNS stimulation
2. Contraindicated with SSRI's or B-agonists |
|
What is the mechanims of selgiline (deprenyl)?
|
pg 312 Selectively inhibits MAO-B, increasing DA
|
|
1.what is the clinical of selgiline (deprenyl)?
2.what is its potential toxicity? |
1.adjunctive agent to L-dopa for Parkinsons.
2.May enhance adverse effects of L-dopa |
|
Analgesics/ Anesthetics
|
pg 312
|
|
General principles
|
pg 312
|
|
What is the significance of drugs with decreased solubility in blood?
|
rapid induction and recovery times . Ie. N20
|
|
What is the significance of drugs with increased solubility in blood?
|
increased potency = I/ MAC. Ie. Halothane
|
|
list the Inhaled Anesthetics?
|
halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide
|
|
What is good about lower solubility?
|
the quicker the anesthetic response, and the quicker the recovery
|
|
What are these drug's effects of inhaled anesthetics such as halothane, enflurane, isoflurane, sevoflurane, methoxyflurane, nitrous oxide?
|
myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow
|
|
What toxicity mactches the following drugs 1. Halothane 2. Methoxyflurane 3. Enflurane 4. Rare
|
1. Hepatotoxcity 2. Nephrotoxicty 3. Proconvulsant 4. Malignant hyperthermia
|
|
What do barbituates, benzodiazepines, arylcyclohexylamines and narcotic analgesics have in common?
|
they are IV anesthetics
|
|
What the pharmacokinetics and uses of thiopental as an IV anesthetic?
|
1. high lipid solubility, rapid entry into brain.
2.Used for induction of anesthesia for short surgical procedures. Terminated by redistribution from brain. Decreased cerebral blood flow |
|
1.What is midazolam(used as an IV anesthetic)?
2.Used for what Tx diagnosis and how it is used? 3.What is this class's shortcoming? |
1. Benzodiazepine
2.midazolam used for endoscopy. Used with gaseous anesthetics and narcotics. 3. May cause severe post-op respiratory depressio and amnesia |
|
What does Ketamine (PCP analog and an arylcyclohexylamine) do?
|
dissociative anesthetic. Cardiovascular stimulant. Causes disorientation, hallucination, bad dreams. Increases cerebral blood flow.
|
|
How are narcotic analgesics used? Examples?
|
Morphone and fentanyl are used with CNS depressant during general anesthesia.
|
|
What is the advantage of propofol- an IV anesthetic?
|
used for rapid anesthesia induction and short procedures. Less post-op nausea than thiopental
|
|
1.Name some esters - Local anesthetics?2.Name some amides?
|
1.procaine, cocaine, tetracaine,
2.lidocaine, bupivacaine, (amides have two I's in name!) |
|
What is the mechanism and clinical use of local anesthetics?
|
1.bind receptor and block Na channels. Tertiary amine local anesthetics penetrate membrane in uncharge form, then bind charged form.
2.Use for minor surgical procedures, spinal anesthesia. |
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How do you decide to use ester or amides?
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if allergic to esters, give amides
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what is the toxicity of Local anesthetics?
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CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, arrhythmias (cocaine: prevents the uptake of NE)
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In infected ________ tissue, anesthetics are charged and cannot penetrate membrane. Therefore, ______ anesthetics are needed.
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acidic; more
Because local anesthetics (esters and amides) are weak bases |
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What is the order of nerve blockade for size and myelination? Which factor predominates?
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small diameter> large diameter. Myelinated fibers> unmyelinated fibers. Size factor predominates
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what is the order of loss of sensation from Local anesthetics?
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pain first, then temp, then touch, then pressure
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Why would you give these drugs with vasoconstrictors?
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to enhance local action
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1.List the opioid drugs?
2.Mechanism? 3. Name the opioid receptors and the drugs that act on them? |
1.morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
2. Opioid receptor agonist 3. mu -morphine delta -enkephalin kappa- dynorphin |
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Clinical use of opioids?
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pain, cough supression (dex), diarrhea (loperamide), acute pulmonary edema, methadone maintenance programs
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What are the major toxicities?
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addiction, respiratory depression, constipation, miosis, additive CNS depression wth other drugs
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1.In Opoid use as an analgesic, Tolerance does not develop to __________and ______
2.How would you treat toxicity? |
1. Miosis and constipation
2.Naloxone, naltrexone (opiod R antagonist) |
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1.List three NSAIDS?
2.What is their mechanism? |
1.ibuprofen, naproxen, indomethacin
2.reversibly inhibit COX 1 and 2. Blocks PG synthesis |
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1.What is their clinical use of NSAIDs(3As)?
2. What is Indomethacin used for? |
1.Antipyretic, analgesic, anti-inflammatory.
2.Indomethacin is used to close a PDA. |
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What are common toxicities of NSAIDs?
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1.Renal damage (reduces the production of PGE in afferent arteriole- poor medullary kidney gets hypoxic)
2.Aplastic anemia, 3.GI distress, 4.Ulcers (COx 1 is important for clearing up and preventing ulcers) |
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Where is cox2 found?
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in inflammatory cells and mediates inflammation and pain
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1.Why is cox2 inhibition better than cox1?
Clinical Use? |
1.Cox1 helps to maintain gastric mucosa, thus, should not have the corrosive effects of other NSAIDs on the GI lining (less incidence of ulcers and bleeding)
2.RA and osteoarthritis |
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1.What is Acetominophen's mechanism and where does it work?
2.What are its 2 As? 3.Overdose effects? |
1.Reversibly inhibits cox, mostly in CNS. Inactivated peripherally.
2.antipyretic, analgesic but NOT anti-inflammatory 3. Hepatic necrosis, acetaminophen metabolites depletes glutathine and forms toxic tissue adducts in the liver |