Week 2: Pharmacology III
Terms
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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
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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)
- Define Sedation?
- Decrease anxiety, motor activity and mental acuity
- Define Hypnosis?
- Drowsiness and increased tendency to sleep
- Are benzodiazepine are they hypnotic, sedative or anxiolytic(or subset of sedative: anxiolytic)?
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Various benzodiazepine have varying properties of all three
Hypnotic, sedative or anxiolytic.
Hypnotic and anxiolytic are popular xteristics -
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 - 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
- how is L-dopa different from dopamine
- L-dopa can cross the blood-brain barrier, dopamine cannot
- what happens to L-dopa after it crosses the BBB
- converted to dopamine by dopa decarboxylase
- what is the function of carbidopa
- peripheral decarboxylase inhibitor
- 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
- 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
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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 - which drugs are used for simple and complex partial seizures
- phenytoin, carbamazapine, lamotrigine, gabapentin, topiramate, phenobarbital
- 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 - what are lamotrigine and topiramate used to treat?
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1.simple and complex partial, tonic-clonic
Topiramate not used for tonic clonic - what types of seizures is gabapentin indicated for
- simple and complex partial, tonic-clonic
- what types of seizures is topiramate indicated for
- simple and complex partial
- what types of seizures is phenobarbital indicated for
- simple and complex partial, tonic-clonic
- what drugs can be used for tonic-clonic seizures
- phenytoin, carbamazapine, lamotrigine, gabapentin, phenobarbital, valproate
- what drugs can be used for absence seizures
- valproate, ethosuximide
- what drugs can be used for status epilepticus
- phenytoin, benzodiazapines (diazepam, lorazepam)
- what types of seizure is valproate indicated for
- tonic-clonic, absence
- what types of seizure is ethosuximide inidcated for
- absence
- what type of seizure are benzodiazepines indicated for
- status epilepticus
- other than anti-seizure, what else is phenytoin used for
- class 1B anti-arrhythmic
- how should a patient taking carbamazepine be followed
- monitor LFT's weekly
- which seizure drugs have adjunct use
- gabapentin, topiramate
- which seizure drug is safest in pregnant women
- phenobarbital
- which seizure drug is used in Crigler-Najjar II
- phenobarbital
- what are the side effects of phenytoin
- nystagmus, diplopia, ataxia, sedation, ginigival hyperplasia, hirsutism, anemias, teratogenic
- what are the side effects of valproate
- GI distress, rare by fatal hepatotoxicity, neural tube defects (spina bifida)
- what are the side effects of lamotrigine
- life-threatening rash, Stevens-Johnson syndrome
- what are the side effects of gabapentin
- sedation, movement disorders
- what are the side effects of topiramate
- sedation, mental dulling, kidney stones, weight loss
- 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
- which anti-epileptic drugs can cause GI distress
- valproate, ethosuximide
- it is necessary to check LFT's with which anti-epileptic drugs
- carbamazepine, valproate
- which anti-epileptic drugs cause CYP induction
- phenobarbital, carbamazepine
- which anti-epileptic drugs can cause blood problems
- carbamazepine, phenytoin
- which anti-epileptic drugs can cause Stevens-Johnson syndrome
- lamotrigine, ethosuximide
- which anti-epileptic drugs can cause diplopia
- carbamazepine, phenytoin
- what is the mechanism of phenytoin action
- use-dependent blockade of Na+ channels
- what is the clinical application of phenytoin
- grand mal seizures
- what are the toxicities of phenytoin
- nystagmus, ataxia, diplopia, lethargy, SLE - drug induced(HIPP)
- what are the chronic toxicities of phenytoin
- gingival hyperplasia in children, peripheral neuropathy, hirsutism, megaloblastic anemia, malignant hyperthermia (rare)
- should pregnant women take phenytoin
- NO -- teratogenic
- Name the drug used in epilespy treatment that can cause megaloblastic anemia?
- Phenytonin
- name 4 barbiturates
- phenobarbital, pentobarbital, thiopental, secobarbital
- 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
- what is the clinical application of barbiturates
- sedative for anxiety, seizures, insomnia, anesthesia induction (thiopental)
- which barbiturate is used for anesthesia induction
- thiopental
- what are the side effects of barbiturates
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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 - what should you find out before giving a patient barbiturates
- what other medications they take, because of CYP induction and many drug interactions
- 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
- when are barbiturates contra-indicated
- porphyria
- name a bunch of benzodiazepines
- diazepam, lorazepam, triazolam, temazepam, oxazepam, midazolam, chlordiazepoxide (all have ZZZ in them)
- what is the mechanism of benzodiazepines
- increase frequency of Cl channel opening --> facilitate GABA-A action (Frenzodiazepines increase frequency)
- which GABA receptors are facilitated by barbiturates and bezodiazepines
- GABA-A
- what are the clinical applications of benzodiazepines
- anxiety, spasticity, status epilepticus (diazepam), detoxification (alcohol withdrawal, DT's)
- which benzodiazepine can be used for status epilepticus
- diazepam
- what drugs can be used to treat alcohol withdrawal
- benzodiazepines
- which benzodiazepines are short-acting
- TOM thumb: Triazolam, Oxazepam, Midazolam
- 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 - are barbiturates or benzodiazepines used for alcohol withdrawal
- benzodiazepines
- what is another name for antipsychotics
- neuroleptics
- name 4 antipsychotic drugs
- thioridazine, haloperidol, fluphenazine, chlorpromazine
- 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)
- what is the mechanism of most antipsychotics
- block dopamine D2 receptors
- what is the clinical application of antipsychotics
- schizophrenia, psychosis
- what are the side effects of antipsychotics
- extrapyramidal side effects (EPS), sedation, endocrine, muscarinic blockade, alpha blockade, histamine blockade
- 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
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evolution of EPS side effects:
4 hours -- acute dystonia,
4 days -- akinesia,
4 weeks -- akasthesia,
4 months -- tardvie dyskinesia - 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 - what type of antipsychotic is clozapine
- atypical
- what type of antipsychotic is olanzapine
- atypical
- what type of antipsychotic is risperidone
- atypical
- 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
- 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 - what test must be done weekly on patients taking clozapine
- WBC count because of potential agranulocytosis
- what is the mechanism of action of lithium
- unknown; may be related to inhibition of phosphoinositol cascade
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what is the clinical application of lithium?
How does it work -
1.mood stabilizer for bipolar disorder
2.Prevents relapse and acute manic episodes - how does lithium help people with bipolar disorder
- prevents relapse and acute manic episodes
- what are the side effects of lithium
- tremor, hypothyroidism, polyuria, teratogenic
- is it OK for women taking lithium to get pregnant
- NO -- teratogenic
- 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
- What are the three C's of their toxicity?
- 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 SSRI toxicity differ from TCA'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
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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
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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?
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1.Hypertensive crisis
non-selective Phenelzine and Tranylcypromine
selective - selegiline - Apart from hypertensive crisis with wine and cheese- What drugs are MAO contraindicated for?
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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
- 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
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What are the effects inhaled anesthetics? (not toxicity effects)
Some inhaled A.: Enflurane,sevoflurane - myocardial depression, respiratory depression, nausea/emesis, increase cerebral blood flow
- What are the three C's of their toxicity of Tricyclic Antidepressants?
- Convulsions, Coma, Cardiotoxicity (arrythmias). Also respiratory depression, hypyrexia.
- 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.
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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
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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?
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1. Mirtazapine. Also potent 5HT-R antagonist.
2. Toxicity - sedation, increase serum cholesterol, increase appetite - What is trazodone? Mechanism? and it' SE?
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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
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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?
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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
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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
- 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?
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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?
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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. - How do you decide to use ester or amides?
- if allergic to esters, give amides
- what is the toxicity of Local anesthetics?
- CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, arrhythmias (cocaine: prevents the uptake of NE)
- 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 - What is the order of nerve blockade for size and myelination? Which factor predominates?
- small diameter> large diameter. Myelinated fibers> unmyelinated fibers. Size factor predominates
- what is the order of loss of sensation from Local anesthetics?
- pain first, then temp, then touch, then pressure
- Why would you give these drugs with vasoconstrictors?
- 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 - Clinical use of opioids?
- pain, cough supression (dex), diarrhea (loperamide), acute pulmonary edema, methadone maintenance programs
- What are the major toxicities?
- 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) -
1.List three NSAIDS?
2.What is their mechanism? -
1.ibuprofen, naproxen, indomethacin
2.reversibly inhibit COX 1 and 2. Blocks PG synthesis -
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. - What are common toxicities of NSAIDs?
-
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) - Where is cox2 found?
- in inflammatory cells and mediates inflammation and pain
-
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 -
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