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134 Cards in this Set

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What are the Secondary amine tricyclic antidepressants?
S-AND
1) Amoxapine
2) Nortryptiline
3) Desipramine

More specific for blocking NE and 5-HT reuptake, so have less side effects than tertiary TCAs.
What are the tertiary amine tricyclic antidepressants?
T-ACID
1) Amitryptiline
2) Clomipramine
3) Imipramine
4) Doxepin

Have more side effects:
1) adrenergic blockade
2) anti-muscarinic (urinary retention, constipation, tachycardia, blurred vision, dry mouth).
3) histamine blocker: sedation
What drug is used for enuresis (bedwetting)?
Imipramine
What drug is used for obsessive compulsive disorder?
Clomipramine.
What are some problems with TCAs and elderly?
Elderly are more sensitive to anti-cholinergic effects, so for them try to use the 2ndary TCA, nortriptyline.
What is the mechanism of action of tricyclic antidepressants?
Inhibit the presynaptic uptake of NE and seretonin.
What are the clinical uses of antidepressants?
Major depression
Bedwetting (Imipramine)
OCD (clomipramine)
Which of the TCAs are least sedating?
Desipramine; good to use in elderly along with nortriptyline.
What is the toxicity of TCAs?
Convulsions
Coma
Cardiotoxicity (arrythmias)
Hyperpyrexia
What are some examples of monoamine oxidase (MAO) inhibitors?
Phenelzine, tranylcypromine
What is the action of MAO inhibitors?
Block MAO which increase levels of NE and 5-HT.
What is the clinical use of phenelzine and tranycypromine?
MAO inhibitor
1) Atypical depression (with psychotic or phobic features)
2) Anxiety
3) Hypochondriasis.
What is contraindicated when taking MAO inhibitors?
1) Tyramine ingestion (because tyramine can stimulate release of NE and Epi) leading to hypertensive crisis
2) Meperidine ingestion (an opioid agonist) --> can lead to hypertensive crisis.
What are some contraindications for MAO inhibitors?
1) Contraindicated with SSRIs
2) Contraindicated with B-agonists

Need to prevent seretonin syndrome

Also contraindicated with tyramine and meperidine.
How long does it take for MAO inhibitors to take effect?
2-4 weeks.

Actually a last choice of antidepressant due to side effects.
What are some examples of SSRIs?
Fluoxetine, Sertraline, paroxetine, Citalopram

Action: serotonin-specific reuptake inhibitors.
What are the clinical uses of SSRIs?
Endogenous depression, OCD, bulimia, and anorexia.
What are the toxicities of SSRIs like fluoxetine, sertraline, paroxetine?
1) Decreased libido with decreased ejaculation
2) CNS stimulation: insomnia
3) Withdrawal effects.
4) Seretonin syndrome with MAO inhibitors: hyperthermia, muscle rigidity, cardiovascular collapse.

**Takes 2-3 weeks for antidepressants to have an effect.
What is fluoxetine?
SSRI
Commonly used for OCD also
Has the longest half life of any of the SSRIs, so withdrawal associated with fluoxetine is less severe.
What is unique about paroxetine?
it is a SSRI that is paradoxically associated with increased activity in the first two weeks of use!
What is indication for buproprion?
1) smoking cessation
2) depression
What is toxicity of buproprion?
Tachycardia, Insomnia due to stimulant effects, headache,

*Seizure in bulimic patients
DOES NOT cause sexual side effects!!
What is action of venlafaxine?
1) Heterocyclic antidepressant
2) Blocks 5-HT, NE, and DA uptake
What is the toxicity of venlafaxine?
Stimulant effect:sedation, nausea, constipation.
What is action of mirtazapine?
1) Alpha-2-antagonist: leads to increase release of NE and 5-HT because it inhibits negative feedback

2) Potent 5-HT2 and 5-HT3 receptor antagonist. *****
What is the toxicity of mirtazapine?
Sedation, increased appetitie.
What is the mechanism of maprotiline?
Blocks NE reuptake. Causes sedation, orthostatic hypotension.

Used for depression.
What is mechanism of action of trazodone?
Primarily inhibit seretonin reuptake: can cause Priapism!!

Used for depression.
What is the use of lithium?
Mood stabilizer for bipolar affective disorder; blocks relapse of acute manic events.
What is the toxicity of lithium?
Tremor, hypOthyroidism, polyuria (ADH antagonist), nephrogenic diabetes insipidus, teratogenesis within 1st trimester.
What is toxicity of lithium?
1) Tremor
2) Nephrogenic diabetes insipidus
3) hypOthyroidism
What is valproic acid used for?
1) bipolar disorder
2) myoclonic seizures
3) absence seizures
What are some side effects of valproic acid?
1) hepatic toxicity
2) rash, alopecia
3) fetal spina bifida
4) Increased bleeding time due to thrombocytopenia.
What is carbamezepine used for?
1) partial and tonic-clonic seizure
2) Trigeminal neuralgia
3) Manic-depressive disorder?
What are some side effects of carbamezepine?
1) Blood dyscrasias (agranulocytosis, aplastic anemia)
2) liver toxicity
3) P450 induction.

**1st line drug for trigeminal neuralgia!!
Which are the atypical antipsychotics?
Clozapine, Olanzapine, and Risperidone
What is the mechanism of action of clozapine, olanzapine, and risperidone?
1) Blocks 5-HT2 and dopamine receptors
What are clozapine, olanzapine, and risperidone used for?
To treat the positive AND negative symptoms of schizophrenia.
What is olanzapine used for?
1) OCD
2) Anxiety disorder
3) Depression, Mania
4) Tourette syndrome
What are some side effects of risperidone?
1) hyperprolactinemia (block dopamine)
2) gynecomastia
3) glactorrhea
4) sexual dysfunction.

Excess prolactin inhibits GnRH.
What is the side effect of clozapine?
Agranulocytosis (requires weekly WBC monitoring).
What are some side effects of olanzapine?
Weight gain and diabetes.
What are some typical antipsychotics?
1) Thioridazine
2) Haloperidol
3) Fluphenazine
4) Chlorpromazine
What are typical antipsychotics used for?
Used to treat the positive symptoms of schizophrenia like delusions, hallucinations, and disorganized speech.
What is the mechanism of action of typical antipsychotics?
Block D2 receptors.
What is the toxicity associated with thioridazine?
Retrograde ejaculation and pigmentation of retina.
What is haloperidol used for?
Tourettes
PCP induced psychosis
huntington's chorea.
What is the toxicity of antipsychotics (neuroleptics)?
Extrapyramidal symptoms
1) Acute dystonia: muscle spasms
2) Akathisia: motor restlessness especially of legs
3) Parkinsonian syndrome
4) Tardive dyskinesia: oral-facial movements (irreversible)
What are some endocrine toxicities of antipsychotics?
Dopamine receptor antangonism --> hyperprolactinemia --> gynecomastia

Also side effects from blocking muscarinic --> dry mouth, constipation.
What is neuroleptic malignant syndrome?
Associated with antipsychotics
1) rigidity
2) myoglobinuria
3) hyperpyrexia
4) altered mental status

Treat with dantrolene or bromocriptine (dopamine agonist).
Explain the evolution of Extrapyramidal side effects in antipsychotics.
4 hours: acute dystonia
4 days: akinesia
4 weeks: akathisia
4months: tardive dyskinesia.
What is Parkinson's disease due to?
1) Loss of dopaminergic neurons
2) Excess cholinergic activity.
What is the action of bromocriptine?
Partial Dopamine agonist
What is action of pramipexole?
Partial Dopamine agonist
What is action of ropinirole?
Partial Dopamine agonist.
What is action of amantadine?
Increases dopamine release
What is action of selegiline?
Prevents dopamine breakdown by selectively inhibiting MAO type B.
What is action of entacapone and tolcapone?
COMT inhibitor

Prevents DA breakdown.
What is action of benztropine?
Antimuscarinic; Used in parkinsons to curb cholinergic excess; improves tremor and rigidity, but has LITTLE effect on bradykinesia (slowness in the execution of movements)!!.
What is mechanism of action of L-dopa/carbidopa?
Increases level of dopamine in the brain.

Unlike dopamine, L-dopa CAN cross the blood-brain barrier and is converted by dopa decarboxylase in the CNS to dopamine.
Why is carbidopa given with L-dopa?
Carbidopa is a peripheral dopa decarboxylase inhibitor, used to increase the bioavailability of L-dopa in the brain and limit peripheral side effects.
What are some side effects of L-dopa (levodopa)?
Peripheral conversion to dopamine can cause arrythmias and postural hypotension.
What is the long-term side effects of L-dopa?
Can cause dyskinesia follwoing administration (difficulty in performing voluntary movements) or akinesia between doses (inability to initiate movements).
What is selegeline mechanism of action?
Inhibits MAO-B, so it increases availability of dopamine.

MAO-A --> oxideizes 5-HT and NE
MAO-B --> oxidizes Dopamine
What is the mechanism of migraines?
1) Release of vasodilatory peptides of cranial blood vessels
2) Increase blood flow associated with dilation causes leakage of plasma and plasma proteins into extracellular space
3) this produces edema
4) mechanical pressure casued by edema --> can stimulate pain receptors in the dura.
What is used to treat migraines?
5-HT agonists because it causes vasoconstriction --> reduces edema and inflammation.

Sumatripan --> 5HT-1 agonist: Use for acute migraine, cluster headache attacks. Should be taken at onset of migraine symptoms because it has half-life of < 2hours.
What is the side effects of sumatripan?
1) Coronary vasospasm, mild tingling (contraindicated in patients with CAD or Prinzmetal's angina).

2) Contraindicated because of the vasospastic effects.
Whats the difference between a simple partial seizure and a complex partial seizure?
Patients do NOT los econsciousness with a simple partial seizures where with a complex partial seizure, patients lose consciousness and will have a postictal period (period of disorientation).
What roles do the benzodiazapenes (diazepam or lorazepam) play in seizures?
1) 1st line agent for status epilepticus
2) Used for seizures of eclampsia (but first line to prevent seizures of eclampsia is MgSO4.)
Waht is mechanism of action of diazepam and lorazepam?
Increases GABA A action.
What are some side effects of benzodiazapenes?
Sedation, tolerance, and dependence.
What role does ethosuxamide play with seizures?
1st line agent for absence seizures.
What is mechanism of action of ethosuximide?
Blocks thalamic T-type Ca++ channels.
What are the side effects of ethosuxamide?
GI distress, urticaria, and Stevens Johnson syndrome: disorder with severe erythema multiforme eruption on skin and lesions of the oral, genital, and anal mucosa, with hemorrhagic crusting on the lips and fever, headache, and arthralgia.
What is valproic acid used for?
All typees of partial seizures
Tonic clonic generalized seizure
Absence seizures, and myoclonic seizures. NOT Used for status epilepticus.
What is mechanism of valproic acid?
1) Increases Na+ channel inactivation
2) Increases GABA concentration.
What are some side effects of valproic acid?
1) Rare but fatal hepatotoxicity (measure LFTs)
2) Neural tube defects (spina bifida in fetus)
3) Tremor, weight gain.
What is phenobarbital used for?
All types of partial seizures, and generalized tonic clonic?

**1ST line in pregnant women, and children.
What is phenobarbital action?
Increases GABA A action.
What is the first line drug for generalized tonic clonic seizures?
Valproic acid.
What is side effect of phenobarbital?
Sedation, tolerance, dependence, and INDUCTION OF CYTOCHROME P450.
What is topiramate used for?
All partial seizures
And generalized tonic clonic
What is mechanism of topiramate?
1) Blocks Na+ channels
2) increases GABA action.
What are some side effects of topiramate?
Sedation, mental dulling, kidney stones, and weight loss.
What is Gabapentin used for?
1) All partial seizures and generalized tonic clonic
2) Used for peripheral neuropathy.
What is gabapentin mode of action?
Increases GABA release.

Side effects: sedation, ataxia.
What is lamotrigine used for?
All partial seizures, tonic clonic generalized seizures.
What is mechanism of action of lamotrigine?
Blcoks voltage-gated Na+ channels.
What is side effect of lamotrigine?
Steven Johnson syndrome.
What is carbamezepine used for?
1st line against generalized tonic-clonic seizures (like valproic acid).

ALSO FIRST LINE FOR TRIGEMINAL NEURALGIA.

WORKS BY INACTIVATING NA+ CHANNELS.
What are some side effects of carbamezepine?
Diplopia, Agranulocytosis, aplastic anemia, liver toxicity, teratogenesis, and induction of P450.
What is mechanism of action of phenytoin?
Use-dependent blockage of Na+ channels;
What is phenytoin used for?
1st line for tonic clonic seizures and 1st line for PROPHYLAXIS of status epilepticus.

2) Also a class IB antiarrythmic.
What is toxicity of phenytoin?
Gingival hyperplasia, hirsutism, megaloblastic anemia (because it interferes with metabolism of Vit B12 which can cause peripheral neurophaty and megaloblastic anemia). Can cause an SLE like syndrome and induction of cytochrome P450. Teratogenic (fetal hydantoin syndrome).
What are some examples of barbituates?
Phenobarbital
Pentobarbital
Thiopental
Secobarbital

All end in "al"
What is mechanism of action of barbituates?
Facilitate GABA A action by increaseing DURATION of CL- channel opening, thus decreasing neuron firing. BARBIDURATES!! (iNCREASED DURATION OF CL- CHANNEL OPENING).
What are barbituates like phenobarbital, pentobarbial, used for?
Sedative for anxiety
Seizures
Insomnia
Induction of anasthesia (thiopental).
What are some toxicities of barbituates?
Dependence
Addictive CNS depression effects with alcohol.
Respiratory or cardiovascular depression.
Induction of P450.
CONTRAINDICATED IN PORPHYRIA!
How do you treat barbituate overdose?
assist respiration
Increase BP.
What are soem examples of benzodiazapenes?
Diazepam, Lorazepam, Traizolam, Temazepam, Oxazepam, midazolam, Alprazolam.
What is mechanism of action of benzodiazapenes?
Facilitate GABA a by INCREASING FREQUENCY OF CL- channel opening. FRENZODIAZAPENES INCREASE FREQUENCY.
What are benzodiazapenes such as diazepam and lorazepam used for?
Anxiety, Spasticity, Status epilepticus (Lorazepam and Diazepam)

Detoxification (especially alcohol withdrawal: Delirium Tremens) Use diazepam.

Used in night terrors and sleep walking.
What are some toxicities of benzodiazapenes?
Dependence
CNS depression effects WITH ALCOHOL.
An overdose of benzodiazapenes alone doesnt cause fatal respiratory depression. however if used in combo with alcohol and barbituates, the CNS depressant effects are potentiated and respiratory depression may occur!!
How do you treat benzodiazapene overdose?
Flumazenil (competitive antagonist at GABA receptor).
What are the short acting benzodiazapenes?
TOM

1) Triazolam
2) oxazepam
3) midazolam
What is effect of anasthetic drugs with decreased blood solubility?
Determined by drug's blood/gas partition coefficient.

Drugs with low solubility dont easily dissolve in blood and therefore reach steady state quickly, causing rapid induction and rapid recovery --> example Nitrous Oxide.

Example: Nitric Oxide: low blood sol
What is effect of anasthetic drug with increased blood solubility?
In blood, reach steady state more slowly, casuing slower induction and recovery. --> example halothane.
What are some examples of inhaled anasthetics?
Halothane, enflurane, isoflurane, methoxyflurane, nitrous oxide. The "ane" drugs.
What are the effects of inhaled anasthetcs like halothane, enflurance, isoflurane, NO?
Myocardial depression
Resp depression
Nausea/Emesis.
Increased cerebral blood flow
Decreased cerebral metabolic demand.
What are the toxicities of halothane?
hepatotoxicity.
What is the toxicity of methoxyflurane?
nephrotoxicity
What is toxicity of enflurane?
Proconvulsant.
What is side effect of inhaled anasthetics though rare?
Malignant hyperthermia: long periods of sustained muscle contractin and with an accompanying rise in body temperatures. It can be treated with a Ca++ channel blocker, dantrolene!!
What is dantrolene used for?
Treat malignant hyperthermia caused by concomitant use of inhalation anasthetics (halothane, isoflurane, etc) and succinylcholine.

Also used to treat neuroleptic malignant syndrome (toxicity of antipsychotic drugs).
What is mechanism of action of dantrolene?
Prevents release of Ca++ from sarcoplasmic reticulum of skeletal muscle.
What are the two classes of neuromuscular blocking drugs?
1) Depolarizing
2) Non-depolarizing

used for muscle paralysis in surgery or mechanical ventilation. Selective for motor nicotinic receptor.
What is succinylcholine used for?
It is used for muscle paralysis in surgery; acts as a neuromuscular blockade drug by acting on depolarization:
1) Phase I (prolonged depolarization): no antidode. Block actually POTENTIATED by cholinesterase inhibitors.

2) Phase II (repolarized but blocked): antidote consists of cholinesterate inhibitors (neostigmine).
What are the nondepolarizing neuromuscular blockade drugs?
Tubocurarine, atracurium, mivacrurium, pancuronium,

Competitive blockage with ACh for receptors.

Reversal of blockage: neostigmine, edrophonium, etc.
What are some intravenous anasthetics?
Barbituates --> Thiopental
Benzodiazapenes --> Midazolam
Ketamine
Opiates --> Morphine, fentanyl
Propofol
What is thiopental used for?
High potency, high lipid solubility, so rapid entry into the brain. Used for induction of anasthesia and short surgical procedure. IT DECREASES CEREBRAL BLOOD FLOW!
What is Midazolam used for?
It is a barbituate

Commonly used drug for endoscopy, used adjunctively with gas anasthetics and narcotics. Can cause severe postoperative depression. Can cause amnesia!! If overdose on midazolam, treat with flumazenil (competitive antagonist at GABA receptors).
What is ketamine used for?
PCP analog that acts as dissociative anasthetic. The dissociative anesthetics uncouple sensory, motor, integrative, memory and emotional activities in the brain, providing there is a functional cerebral cortex. The state induced by high doses of ketamine is best described as catalepsy and is not accompanied by central nervous system depression. There is depression of respiratory function, but cardiovascular function is maintained. Muscle relaxation is very poor. It is a cardiovascular stimulant, causes disorientation, hallucination, and ad dreams. INCREASES CEREBRAL BLOOD FLOW.
What are morphine and fentanyl used for?
Used during general anasthesia with other CNS depressants.
What is propofol used for?
Rapid anasthesia induction and short procedures.
ketamine
Used for kids.
What is rht eorder of sensation loss with anasthetics?
1) Pain
2) Temperature
3) Touch
4) Pressure.
What are the types of local anasthetics?
1) Esters --> procaine, cocaine, tetracaine

2) Amides: idocaine, mepivicaine, bupivicaine: Amides have 2 I's in name!!
What is mechanism of local anasthetics?
Blocks Na+ channels by binding to specific receptor on inner portion of channel.
Do you need more or less local anasthetic in infected tissue?
You need more because infected tissue is acidic, so anasthetics are charged and cannot penetrate membrane effectively.
Which nerve fibers are blocked with more force?
small diameter fibers > large diameter

Myelinated fibers > unmyelinated.

So smaller, myelinated fibers blocked more effectively.

Overall size factor predominates, so small unmyelinated pain fibers > small myelinated autonomic fibers > large myelinated autonomic fibers.
What is the order of loss of sensation?
1) Pain
2) Temperature
3) Touch
4) Pressure.
Why is epinephrine (vasoconstrictor) given with local anasthetics?
To enhance local action, decrease bleeding, and increase anasthesia by decreases systemic concentration and keeping the drug localized!
What are some side effects of cocaine?
arrythmias (cocaine).
What are the side effects of the amide bupivacaine?
severe cardiovascular toxicity