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162 Cards in this Set

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What is the NT effect that causes parkinsons?
1) Decrease Dopamine
2) Increased acetylcholine
Which drugs are ergot alkaloids used to treat Parkinsons?
Bromocriptine and pergolide.

Both agonize dopamine receptors.
What class of drugs are non-ergot dopamine receptor agonists?
Pramipexole

Ropinirole
What is the action of bromocriptine?
Dopamine receptor agonist: ergot alkaloid
What is action of pergolide?
Dopamine receptor agonist: ergot alkaloid
What is pramipexole used for?
Dopamine receptor agonist: non ergot alkaloid to treat Parkinsons.
What is ropinirole used for?
Dopamine receptor agonist: non-ergot alkaloid.
What is the action of amantadine?
Increases dopamine release.
What is MAO of entacapone?
Blcoks COMT, so cant convert Levodopa to 3-OMD, so more levodopa available for brain.
What is MAO of talcapone?
Blcoks COMT, so cant convert Levodopa to 3-OMD, so more levodopa available for brain.
What is benzotropine action?
Antimuscarinic
What can benzotropine improve in parkinsons patients?
Improve Tremor and Rigidity
What does benzotropine not improve in parkinsons patients?
Bradykinesia.
What is action of L-dopa?
Increases dopamine in the brain. L dopa can cross the BBB (unlike dopamine).
Why is carbidopa given with L-dopa?
Carbidopa prevnents the dopa decarboxylase in periperhy. Therefore more Dopa can reach the brain.
What are the side effects from peripheral conversion of levodopa to dopamine?
1) Tacchyarythmias
2) Postural HTN
3) Hot flashes
4) Nauses: dopamine stimulates emetic center (which is OUTSIDE BBB).

**Can decrease these peripheral side effects by adding peripheral decarboxylase inhibitor?
What dopamine drugs side effects will continue even with peripherala decarboxylase inhibitor?
Anxiety and Agitation. Actually peripheral dopa decarboxylase inhibitors can increase the side effects.
What is side effect of L-dopa/Carbidopa after long use?
Dyskinesia following administration.

Akinesia between doses.
Wahat is MOA of selegiline?
Inhibits MAO-B. Normally MAO B oxidizes dopamine.
What are the side effects from peripheral conversion of levodopa to dopamine?
1) Tacchyarythmias
2) Postural HTN
3) Hot flashes
4) Nauses: dopamine stimulates emetic center (which is OUTSIDE BBB).

**Can decrease these peripheral side effects by adding peripheral decarboxylase inhibitor?
What dopamine drugs side effects will continue even with peripherala decarboxylase inhibitor?
Anxiety and Agitation. Actually peripheral dopa decarboxylase inhibitors can increase the side effects.
What is side effect of L-dopa/Carbidopa after long use?
Dyskinesia following administration.

Akinesia between doses.
Wahat is MOA of selegiline?
Inhibits MAO-B. Normally MAO B oxidizes dopamine.
What is MOA of sumatripan?
5-HT1 agonist. Causes vasoconstriction, so reduces edema and inflammation.

Used in acute migraine, cluster headaches.
In what patients are sumatripan contraindicated in?
CAD patients or those with Prinzmetals angina, because it can cause coronary vasospasm.
What is the treatment of choice for absence seizures?
Ethosuximide

2. Sodium valproate
What is MOA of ethosuximide?
Blocks thalamic T type Calcium channels.
What is the side effect of ethosuximide?
GI distress
Urticaria
Stevens Johnson Syndrome!
What is the MAO of the 1st line agent used to treat partial seizures, both simple and complex?
Increases the Na+ channel inactivation : Carbamezapine.
What is mechanism of action for the drug that can treat brief arrythmic jerkin movement lasting <1 sec that occur in in clusters with NO loss of consciousness?
Myocolonic Seizures:

Valproic Acid:

Increase NA channel inactivation AND Increases GABA concentration.
What drug is 1st line for trigeminal neuralgia?
Carbamezepine:
What is action of carbamezepine?
Increases Na+ channel inactivation.
What are the first line agents for tonic clonic general seizures?
Phenytoin
Carbamezepine
Valproic Acid
What is the first line agent for prophylaxis of status epilepticus??
Phenytoine (only after IV diazepam is given for acute symptoms), then phenytoin for prevention.
In a pregnant woman which seizures, what is the mechanism of the drug that is a first line agent?
Increases GABA a action: phenobarbital!!
What is the first line agents to treat seizures in children? Pregnant women?
Phenobarbital.
What is the first line agenf roa acute status epilepticus?
Benzodiazapnes (IV lorazepam or IV diazepam).
What is topiramate used for?
Seizures: Blocks Na+ channels and Increases GABA action.
What is MOA of lamotrigine?
Blocks Na+ channels.
What is side effect of the anti seizure medication topiramate?
1) Sedation
2) Mental dulling
3) kidney stones
What is MOA of Gabapentin?
Actually increases GABA release!

Used to treat peripheral neuropathy as well.
What is the most common side effect of carbamazepine?
Blood dyscrasias: agranulocytosis, aplastic anemia.

Induction of cytochrome p450.
What are the toxicities of ethosuximide?
Stevens Johnson syndrome, urtricaria.
Induce or inhibit P450?

Phenobarbital
Induce
Induce or inhibit P450?
Phenytoin
Induce or inhibit P450?
Rifampin
Induce or inhibit P450?
carbampezepine?
induce
Induce or inhibit P450?
Alcohol
induce
Induce or inhibit P450?
Cimetidine
Inhibit
Induce or inhibit P450?
Erythromycin
Inhibit
Induce or inhibit P450?
Ciprofloxacin
Inhibit
Induce or inhibit P450?
carbampezepine?
induce
Induce or inhibit P450?
Alcohol
induce
Induce or inhibit P450?
Cimetidine
Inhibit
Induce or inhibit P450?
Erythromycin
Inhibit
Induce or inhibit P450?
Ciprofloxacin
Inhibit
Inhibitors or inducer of P450?
Grapefuit juice?
inhibitor
Induce or inhibit P450?
Ritonivir
Inhibit
Induce or inhibit P450?
Isoniazid?
Inhibit
Induce or inhibit P450?

Azole antifungals?
Flucanozole
What are side effects of phenytoin?
CNS: ataxia nystagmus due to cerebellar effects

Gingival hyperplasia, hirsutism

Interferes with Vit B12: megaloblastic anemia

Increases cytochrome P450

SLE syndrome
Side effects of valproic acid?
Hepatotoxicity (check LFTs)

Neural tube defects in children (spina bifida)
Side effect of lamotrigine?
Stevens Johnsons syndrome.
What is mechanism of action of phenytoin?
Blockage of Na+ channels by increasing Na+ channel inactivation. Also inhibits glutamate release from presympatic neuron.
What is phenytoin used for?
1st line agent for tonic clonic generalized seizures.

1st line for prophylaxis of status epilepticus!
This drug used for seizures can cause megaloblastic anemia?
Phenytoin
This drug can cause induce cytochrome P450 AND cause hirsutism?
Phenytoin
This drug can cause gingival hyperplasia in children and peripheral neuropathy?
Phenytoin
What is MOA of phenobarbital?
Binds to GABA a receptor and increases DURATION of Cl- channel opening, and thus decreasing neuron firing!
What is MOA of thiopental?
Binds to GABA a receptor and increases DURATION of Cl- channel opening, and thus decreasing neuron firing!
What is MoA of pentobarbital?
Binds to GABA a receptor and increases DURATION of Cl- channel opening, and thus decreasing neuron firing!
What is MOA of secobarbital?
Binds to GABA a receptor and increases DURATION of Cl- channel opening, and thus decreasing neuron firing!
What disease is pentobarbital contrindicated in?
Porphyria
What is the clinical use of phenobarbital?
1st line agent for seizures in pregnant women and children!

Insomnia, Anxiety
What effect does barbituates have on P450?
Increases p450
This drug has additive CNS depressio effects with alcohol?
Phentobarbital

Benzodiazapenes
What are side effects of phenobarbital?
dependence

additive CNS depression with alcohol

Respiratory or cardiovascular depression (can lead to death).
Treatment of this drug overdose requires symptoms managemetn: assist in respiration and increase the BP?
Barbituates
What is MOA of diazapam?
Binds to GABA a receptor and facilitates frequency of CL- channel opening.
What is MOA of lorazepam?
Binds to GABA a receptor and facilitates frequency of CL- channel opening.
What is MOA of chlordiazepoxide?
Binds to GABA a receptor and facilitates frequency of CL- channel opening.
These drugs work by binding to the GABA a receptor?
Benzodiazapenes
Barbituates
Zolpidem
Alcohol
What is use of lorazepam/diazapem
1) Treat alcohol withdrawal: delirium tremens

2) Acute treatment for status epilepticus!

3) Night terrors
4) Sleepwalking
What is use of lorazepam and diazapem?
1) Anxiolytic
2) Muscle relaxant
3) Anti-convulsant.
What are the short acting benzodiazapenes?
Triazolam

Oxazepam

Midazolam
How do you treat an overdose of lorazepam?
Flumenazil which is a competitive antagonist of GABA receptor.
What is MOA of fluphenazine?
Block dopamine D2 receptors.
Thioridazine MOA
Block dopamine D2 receptors.
Haloperidol MOA
Block dopamine D2 receptors.
Chlorpromazine MOA
Block dopamine D2 receptors.
What is thioridazine, haloperidol used for?
Schizophrenia
Psychosis
Acute mania
Tourette syndrome (haloperidol)
What is toxicity of chlorpromazine?
extrapyramidal side effects
antimuscarinic side effects
anti-adrenergic side effects
anti-histamine side effects.
What is toxicity of thioridazine?
extrapyramidal side effects
antimuscarinic side effects
anti-adrenergic side effects
anti-histamine side effects.
What is toxicity of haloperidol?
extrapyramidal side effects
antimuscarinic side effects
anti-adrenergic side effects
anti-histamine side effects.
What drugs can cause pigmentation of retina and retrograde ejaculation?
Thioridazine
A patient comes in with generalized rigidity , myoglobinuria, hyperpyrexia, and autonomic instability. What medication are they on?
Thioridazine
Haloperidol
fluphenazine

Neuroleptic malignant syndrome.
How do you treat a patient with neuroleptic malignant syndrome?
Dantrolene

or Bromocriptine.
A patient comes in taking a medication is discovered to have gynecomastia and hyperprolactinemia? What drug?
Dopamine antagonist: haloperidol, fluphenazine, thioridazine, chloropromazine.
A patient comes in with involuntary biting, chewing, grimacing and tongue protrusions? What drug his he/she on?
Antipsychotics: thioridazine, haloperidol, etc.

Tardive dyskinesia: involuntary perioral movements, biting, chewing, grimacing, tongue protrusions that are irreversible: starts around 4 months after medication taking.
What are the non extrapyramidal effects of antipsychotics?
1) Dry mouth, constipation: antimuscarinic
2) Sedation: anti histmine
3) Hypotension: anti-adrenergic
Please explain the evoluation of EPS side effects of haloperidol, thirodizaine?
4 hours: acute dystonia: twisting involuntary movements and abnormal posture

4 days: akinesia: inability to initiate movement.

4 weeks: akathisia: "feeling on edge" unable to sit in one position. Restless leg

4 months: tardive dyskinesia!
What is mechanism of clozapine?
Atypical antipsychotic

Blocks 5-HT2 and dopamine receptors.
What is mechanism of risperidone?
Atypical antipsychotic

Blocks 5-HT2 and dopamine receptors.
What is mechanism of olanzapine?
Atypical antipsychotic

Blocks 5-HT2 and dopamine receptors.
This drug is used for OCD, anxiety disorders?
Olanzapine
What is good use of clozapine, olanzapine in treatment of schizophrenia?
Both positive and negative symptoms!
This drug used to treat schizophrenia can ause agranulocytosis?
Clozapine!
this drug is thought to be related to inhibition of phosphoinositol cascade?
Lithium.
This drug is used for bipolar disease
Lithium.
This drug can cause hypothyroidism and movement tremors?
Lithium.
This drug can cause polyuria and hypothyroidism?
lithium.
What is side effect of Lithium?
Nephrogenic diabetes insipidus
Hypothyroidism
Pregnancy Problems.
What drugs are contraindicated with Lithium?
Thiazide diuretics and metronidazole. Lithium is almost exclusively filtered by the kidney, so most of the filtered lithium is reabsorbed in proximal tubule. Thiazide diuretics cause volume, depletion, so kidneys try to retain Na+ in proximal tubule, and then in menatime reabsorb lithium as well! Same thing goes for NSAIDs! same reason with NSAIDs are contraindicated in CHF: because kidney think there is volume depletion due to inhibition of prostaglandins.
What is fluoxetine?
SSRI: used to treat depression
What is sertraline?
SSRI: used to treat depression
What is paroxetine?
SSRI: used to treat depression;
Block Reuptake of 5-HT ino the presynaptic neuron, so remains in the cleft to activate postsynaptic neuron.
What is the side effects of sertraline?
Anorgasmia (Sexual dysfunction)
What are side effects of paroexetine?
Anorgasmia (Sexual dysfunction)
What drug is fluoxetine absolutely contraindicated against?
MAO inhibitors: can lead to seretonin syndrome: hyperthermia, rigidity of muscle, and cardiovascular collapse.
How long does it take fluoxetine to be effectivee?
2-3 weeks
What class of drugs is imipramine?
Tricyclic antidepressants
What are the tertiary amine tricyclics?
T-ACID
1) Amitryptyline
2) Clomipramine
3) Imipramine
4) Doxepin
What are the secondary amine tricyclics?
S-AND
1) Amoxapine
2) Nortryptiline
3) Desipramine
What is mechanism of action of imipramine?
Blocks reuptake of NE and 5-HT
What is mechanism of amitryptiline?
Blocks reuptake of NE and 5-HT
What is mechanism of clomipramine?
Blocks reuptake of NE and 5-HT
What is mechanism of desipramine?
Blocks reuptake of NE and 5-HT W
What is mechanism of nortryptiline?
Blocks reuptake of NE and 5-HT
What is the drug used to treat bedwetting?
Imipramine
What drug can be used to treat OCD?
Clomipramine
What is the toxicity of amitryptiline?
1) Cardiotoxicity (arrythmias)
2) Anticholinergic side effect
3) Sedation
4) Alpha blocking effects
What is toxicity of imipramine?
1) Cardiotoxicity (arrythmias)
2) Anticholinergic side effect
3) Sedation
4) Alpha blocking effects
When using a tricyclic antidepressant, what drug should be used to treat the elderly? Why?
Notryptiline: because it has less of an antimuscarinic effect , so can help revent confusion and hallucinations!!
This drug is a nonselective MAO inhibitor?
Phenelzine
This drug is a nonselective MAO inhibitor?
Tranylcypromine
This drug is used to treat atypical depression: weight gan, increased sleep, psychotic, or phobic features? Anxiety
Phenelzine. (MAO inhibitor).
What is side effect of phenelzine?
Cannot eat with cheese and wine, beecause these agents contain tyramine which displace NE from terminals and increase hypertension.
What drugs are phenelzine contraindicated with?
Meperidine (opiod analgesic)!

SSRIs --> seretonin syndrome

Beta agonist --> HTN.
This drug is used for smoking cessation and depression.
Buproprion.
This drug does NOT cause sexual side effects, so can be used in depression.
Buproprion.

If SSRIs causing problems, convert to buproprion.
This drug is contraindicated in bulimic patients because it leads to seizures.
Buproprion --> leads to seizure
This drug is used in general anxiety disorder and is a heterocyclic antidepressant?
Venlafaxine.
This depressant is an alpha-2- agonist.
Mirtrazapine: inccreases release of NE and 5-HT.
What is side effect of mirtrazapine?
Sedation, Weight gain, Elevated serum cholesterole.
What is MOA of maprotiline?
It is a heterocyclic antidepressant

Blcoks NE reuptake.
Which heterocyclic antidepressant can cause priapism?
Trazodone. It blocks 5-HT uptake.
In relation to anasthetics, what effect will drugs with low solubility in blood have?
Rapid induction and rapid recovery times.
What effect will drugs with high solutilibyt in lipids have in relation to anasthetics?
Decrease MAC

Increased potency!!
Which drug has a low solubility in blood and low solubility in lipid? It is an anasthetic
N20: so fast induction and low potency.
Which drug has high lipid solubility and high blood solubility?
Halothane: slow onset and high potency.
What are some inhaled anasthetics?
Halothane
Enflurane
Isoflurane
Nitrous oxide
This inhaled anasthetic can cause hepatic necrosis
Halothane
This inhaled anasthetic can cause nephrotoxicity
Methoxyflurane
What effect do inhaled anasthetics have on blood flow?
Increases cerebral blood flow
What effect do inhaled anasthetics have that can be a major problem?
Malignant Hyperthermia.
This barbituate is used as an IV anasthetic?
Thiopental. --> high potency, high lipid solubility, and rapid entry into brain.
This drug is rapid entry into the brain, is a barbituate, has high lipid solubility and high potency. Used for short surgical procedures.
Thiopental. THIOPENTAL DECREASES BLOOD FLOW WHERES INHALED ANASTHETIC INCREASE IT.
This benzodiazapene is commonly used to endoscopy procedures as anasthetic?
Midazolam
This drug is a PCP analog that acts as a dissociative anasthetic
Ketamine
This drug is a cardioavascular stimulant, causes disorientation, hallucination, and bad dreams. Completely uncouples motor, sensory, integration activities of brain
Ketamine. Increases cerebral blood flow.
Propofol
Rapid anasthesia induction.
What is the order of sensation loss?
1) Pain
2) Temp
3) Touch
4) Pressure