Week 2: Pharmacology III

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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
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)?: 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
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
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
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
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
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?: 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
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: 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
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
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
is tardvie dyskinesia reversible: often irreversible
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
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
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
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
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
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
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.
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
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.
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.: 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
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
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

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