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228 Cards in this Set

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  • Back
glaucoma drugs
p. 307
which alpha agonists are used to treat glaucoma
epinephrine, brimonidine
which beta blockers are used to treat glaucoma
timolol, betxolol, carteolol
which cholinomimetics are used to treat glaucoma
pilocarpine, carbachol, physostigmine, echothiophate
which diuretics are used to treat glaucoma
acetazolamide, dorzolamide, brinzolamide
which prostaglandin is used to treat glaucoma
latanoprost
what classes of drugs are used to treat glaucoma
alpha agonists, beta blockers, cholinomimetics, diuretics, prostaglandins (*mnemonic -- treating glaucoma is easy as ABCD)
what is the effect of epinephrine in glaucoma
increase outflow of aqueous humor
what are the side effects of epinephrine treatment in glaucoma
mydriasis, stinging
what glaucoma should epinephrine NOT be used for
closed-angle glaucoma
what is the effect of brimonidine in glaucoma
decreased aqueous humor synthesis
what are the side effects of brimonidine treatment in glaucoma
no pupillary or vision changes
what is the effect of beta-blocker treatment in glaucoma
decrease aqueous humor secretion
what are the side effects of beta blocker treatment in glauzoma
no pupillary or vision changes
what is the effect of cholinomimetics in glaucoma
ciliary muscle contraction, opening of trabecular meshwork, increase outflow of aqueous humor
what are the side effects of cholinomimetics in glaucoma
miosis, cyclospasm
what is the effect of diuretic treatment in glaucoma
inhibition of carbonic anhydrase --> decrease HCO3 secretion --> decrease aqueous humor secretion
what are the side effects of diuretics in glaucoma
no pupillary or vision changes
what is the effect of prostaglandin (latanoprost) treatment in glaucoma
increase outflow of aqueous humor
what is the side effect of prostaglandin treatment in glaucoma
darkens color of iris (browning)
which drugs used to treat glaucoma increase outflow of aqueous humor
cholinomimetics, prostaglandin, epinephrine
can you use epinephrine in closed-angle glaucoma
NO
brimonidine is used to treat what eye disease
glaucoma
what kind of drug is latanoprost
prostaglandin
latanoprost is used to treat what eye disease
glaucoma
which glaucoma drugs decrease aqueous secretion
beta blockers, diuretics
L-dopa/carbidopa
p. 307
what does L-dopa stand for
levodopa
what is the mechanism of action of L-dopa/carbidopa
increase dopamine level in brain
what is L-dopa/carbidopa used to treat
Parkinson's disease
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 enzyme convertes L-dopa to dopamine
dopa decarboxylase
what is the function of carbidopa
peripheral decarboxylase inhibitor
why is carbidopa given with L-dopa
increase L-dopa availability in CNS by inhibiting decarboxylase in periphery, also limits peripheral side effects
what are the side effects of L-dopa.carbidopa treatment
arrhythmias, dyskinesias
why do patients taking L-dopa get arrhythmias
peripheral effects of dopamine
why do patients taking L-dopa get dyskinesias
excess dopamine stimulation in CNS
Parkinson's disease drugs
p.308
what drugs are used to treat Parkinson's disease
dopamine agonists, MAO inhibitors, antimuscarinics
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
selegiline
what is the mechanism of selegiline
selective MAO type B inhibitor
what antimuscarinic is used to treat Parkinson's
benztropine
what is the effect of benztropine in Parkinson's
improves tremor, rigidity, little effect on bradykinesia
Sumatriptan
p. 308
what is sumatriptan used for
acute migraine, cluster headache attacks
what is the mechanism of sumatriptan
5-HT1D agonist
what is the half life of sumatriptan
less than 2 hours
what are the side effects of sumatriptan
chest discomfort, mild tingling
what are the contraindications for sumatriptan
patients with CAD or Prinzmetal's angina
Epilepsy drugs
p. 308
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
what types of seizures is carbamazepine indicated for
simple and complex partial, tonic-clonic
what types of seizures is lamotrigine indicated for
simple and complex partial, 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 advantages of phenobarbital
can be used in pregnant women, Crigler Najjar II
Epilepsy drug toxicities
p. 309
what are the side effects of benzodiazepines
sedation, tolerance, dependence
what are the side effects of carbamazepine
diplopia, ataxia, CYP induction, blood dyscrasias, liver toxicity
what are the side effects of ethosuximide
GI distress, lethargy, headache, urticaria, Stevens-Johnson syndrome
what are the side effects of phenobarbital
sedation, CYP induction, tolerance, dependence
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
Phenytoin
p. 309
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
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
why does phenytoin cause megaloblastic anemia
causes decreased vitamin B-12
Barbiturates
p. 309
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
increase duration of Cl channel opening which decreases neuron firing (Barbidurate increases duration
is barbiturate action on the CNS stimulatory or inhibitory
inhibitory
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
dependence, additive CNS depression effects with alcohol, respiratory or CV depression (death), 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
can barbiturates cause dependence
YES
My friend Barb was very anxious so her doctor gave her barbiturates to increase the duration of the time she could speak in public without freaking out and having a seizure. She became so dependent on it that she recommended it to her friend Portia who couldn't take it because of porphyria. One day Barb drank too much alcohol and took her barbiturates and never woke up! THE END
clinical pharmacology made ridiculous. Period
Benzodiazepines
p. 309
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
what are the toxic effects of benzos
dependence, additive CNS depression effects with alcohol
how are benzos better than barbiturates
less respiratory depression and coma risk
how do you treat benzo overdose
flumazenil
what is flumzenil used for
benzo overdose
how does flumazenil work
competitive antagonist at GABA receptor
can a patient become benzodiazepine dependent
YES
are barbiturates or benzodiazepines used for alcohol withdrawal
benzodiazepines
Antipsychotics (neuroleptics)
p. 310
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
a side effect of antipsychotics; rigidity, autonomic instability, hyperpyrexia
how do you treat neuroleptic malignant syndrome
dantrolene, dopamine agonists
what is tardive dyskinesia
side effect of neuroleptics; stereotypic oral-facial movements, may be due to dopamine receptor sensitization
what is the "rule of 4" with EPS side effects from antipsychotic drugs
evolution of EPS side effects: 4 hours -- acite dystonia, 4 days -- akinesia, 4 weeks -- akasthesia, 4 months -- tardvie dyskinesia
is tardvie dyskinesia reversible
often irreversible
what is fluphenazine used for
schizophrenia, psychosis
Atypical antipsychotics
p. 310
name 3 atypical antipsychotics
clozapine, olanzapine, risperidone
what type of antipsychotic is clozapine
atypical
what type of antipsychotic is olanzapine
atypical
what type of antipsychotic is risperidone
atypical
what is the mechanism of atypical antipsychotics
block 5-HT2 and dopamine receptors
what is the mechanism of clozapine
block 5-HT2 and dopamine receptors
what is the mechanism of olanzapine
block 5-HT2 and dopamine receptors
what is the mechanism of risperidone
block 5-HT2 and dopamine receptors
what is the clinical application of clozapine
schizophrenia positive and negative symptoms
what is the clinical application of olanzapine
schizophrenia positive and negative symptoms, OCD, anxiety disorder, depression
what is the clinical application of risperidone
schizophrenia positive and negative symptoms
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 to treat positive and negative symptoms of schizophrenia
atypical ones -- clozapine, olanzapine, risperidone
which antipsychotics should be used for fewer side effects
atypical ones -- clozapine, olanzapine, risperidone
what is a potential toxicity of clozapine
agranulocytosis
which antipsychotic drug can cause agranulocytosis
clozapine
what test must be done weekly on patients taking clozapine
WBC count because of potential agranulocytosis
Lithium
p. 310
what is the mechanism of action of lithium
unknown; may be related to inhibition of phosphoinositol cascade
what is the clinical application of lithium
mood stabilizer for bipolar disorder
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
Antidepressants
pg 311
What do the following drugs inhibit: 1. MAO inhibitors, 2. Desipramine/maprotilline, 3. Mirtazapine and 4. Fluoxetine/trazodone?
1. MAO 2. NE reuptake 3. Alpha 2-R 4. 5HT reuptake
All of the above actions are ------synaptic
PRE
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 does the toxicity 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
Which one is used for smoking cessation?
Buproprion. Mechanism not known. Toxicity - stimulant effects, dry mouth, aggrevation of pyschosis
Which one used in GAD?
Venlafaxine - inhibits 5HT and DA reuptake. Toxicity - stimulant effects
which one blocks NE reuptake
maprotiline
Which one increases release of NE and 5HT via alpha 2 antagonism?
mirtazapine. Also potent 5HT Rantagonist. Toxicity - sedation, increase serum cholesterol, increase appetite
What is trazodone and it' SE?
primarily inhibits seratonin reuptake. Toxicity - sedation, nausea, priapism, postural hypotension
Give 2 examples of MAO
pg 312 phenelzine. Tranylcypromine
Mechanism and Clinical Uses?
non selevtive MAO inhibition. Atypical antidepressant, anxiety, hypochondriasis
What is the toxicity with tyramine ingestion (in foods) and meperidine?
Hypertensive crisis
Other toxicities?
CNS stimulation, contraindicated with SSRI's or B-agonists
What is the mechanims of selgiline (deprenyl)?
pg 312 Selectively inhibits MAO-B, increasing DA
what is the clinical use and toxicity?
adjunctive agent to L-dopa for Parkinsons. 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
Inhaled Anesthetics
pg 312
list them
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?
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
IV anesthetics
pg313
What do barbituates, benzodiazepines, arylcyclohexylamines and narcotic analgesics have in common?
they are IV anesthetics
What the pharmacokinetics and uses of thiopental?
high lipid solubility, rapid entry into brain. Used for induction of anesthesia for short surgical procedures. Terminated by redistribution from brain. Decreased cerebral blood flow
Give an example of a benzo and what is this class's shortcoming?
midazolam used for endoscopy. Used with gaseous anesthetics and narcotics. 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
used for rapid anesthesia induction and short procedures. Less post-op nausea than thiopental
Local anesthetics
pg 313
Name some esters?
procaine, cocaine, tetracaine,
Name some amides?
lidocaine, bupivacaine, (amides have two I's in name!)
What is the mechanism and clinical use?
bind receptor and block Na channels. Tertiary amine local anesthetics penetrate membrane in uncharge form, then bind charged form. 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
CNS excitation, severe cardiovascular toxicity (bupivacaine), hypertension, arrhythmias (cocaine)
In infected ________ tissue, anesthetics are charged and cannot penetrate membrane. Therefore, ______ anesthetics are needed.
acidic; more
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?
pain first, then temp, then touch, then pressure
Why would you give these drugs with vasoconstrictors?
to enhance local action
Opiod analgesics
pg 313
List as many as you can.
morphine, fentanyl, codeine, heroin, methadone, meperidine, dextromethorphan
Mechanism: They act as _____ for opiod receptors to modulate synaptic transmission
agonists
which drugs act at the mu, delta, kappa receptors?
morphine enkephalin, dynorphin
Clinical use?
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
Tolerance does not develop to __________and ______
miosis and constipation
How would you treat toxicity?
naloxone, naltrexone (opiod R antagonist)