A - S1 Cns Pharmacology Imsa

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intermediate acting benzodiazepine used for the txmt of panic disorders

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alprazolam

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2 benzodaizepine drugs which have seditive effects and cause physical dependence

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alprazolam and clonazepam

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drug which binds 5-HT1A receptors with minimal abuse potential

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buspirone

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used in the management of depression, it inhibits the reabsorption of both norepinephrine and serotonin with the synapse

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amitriptyline
nortiptyline
imipramine
desipramine

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drug used to tx nocturnal enuresis

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imipramine

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major se include:
sedation
orthostatic hypotension
cardiac arrhythmias

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tricyclic anit-depressants

amitriptyline
nortriptyline
imipramine
desipramine

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drug class?

amitriptyline
nortriptyline
imipramine
desipramine

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tricyclic anit-depressants

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orally active antispasmolytic agent

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baclofen

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GABA-B receptor agonist that fxn on inhibitory pathways in the spinal cord

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baclofen

Front 10

bc of its low toxicity this local anesthetic can be used on large surface areas adn is available otc as an ointment

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benzocaine

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benzocaine
cocaine
procaine

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3 ESTER local anesthetics

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lidocaine
bupivacaine
ropivacine

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3 AMIDE local anthetics

Front 13

uses to releive pain and itch, also to lubricate medical devices

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benzocaine

Front 14

causes contact sensitizations than other local anesthetics
-rapid onset (1 min) and last for 15 - 20 min

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benzocaine

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antimuscarinic used in management of parkinson disease, improving tremors and rigidity, but does little for bradykinesia

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benztropine
trihexyphenidyl

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low doese may be useful for early onset of tremor, rigity, and drooling

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benztropine

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blocks neurochemical imbalance in striatum due toloss of dopamine

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benztropine

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cns se:
-impaired memory
-drowsiness
-confusion
-delusions

peripheral se:
-dry mouth
-blurred vision
-urinary retention
-tachycardia

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benztropine

Front 19

contraindicates include:
-prostatic hyperplasia
-GI obstruction
-closed-angel glaucoma

these are more common in older pt

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all antimuscarinics including benztropine

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drugs ues to tx parkinson disease as well as in the tx of prolactinoma

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bromocriptine

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ergot derivative acts as D2 agonist, improves estrapyramidal fxn and also inhibits the release of prolactin from pituitary gland

-no longer used bc of se

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bromocriptine

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long acting amide-type local anesthetic can cause severe hypotension and arrhythmias if inadvertently given iv

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bupivacine

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potent and cardiotoxic due to Na channel and reduced cardiac contractility

-produces sensory analgesia with little or no motor impairment

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bupivacine

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local anesthetic binds to sodium channels in the open and inactive state, slowing recovery from depolarization 10 to 1000 fold

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bupivacine

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antidepressant used in the management of nicotine withdrawal in pt seeking to stop cigarette smoking with minimal sedation

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bupropion

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2nd generation hetrocyclic antidepressant inhibits the reuptake of norepinephrine

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bupropion

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3rd generation antidepressant which inhibits reuptake of serotinin

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venlafaxine

Front 28

agent used in txmt of partial and generalized seizures, and is the primary agent used in the txmt of trigeminal neuralgia

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carbamazepine

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anti-seizure medication that may exacerbate myoclonic and absence seizures

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carbamazepine

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antiseizure drug?

moa: inhibits Na channels on neurons

-extensive hepatic cyp 3A4 metabolism to ACTIVE epoxide metabolite, significant microsomal induction

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carbamazepine

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must moniter for:
1. leuckopenia
2. hyponitremia
3. rash -> steven johnson syndrome = burn like rash
4. liver enzymes

-its use may result in idiosyncratic blood disorders such as aplastic anemia and agranulocytosis

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carbamazepine

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second line txmt for schizophrenia that is better for negative symptoms of diseases

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clozapine

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atypical antipsychotic associated with agranulocytosis that blocks D4 receptor

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clonzapine

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only local anesthetic with vasoconstrictor activity

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cocaine

Front 35

used for anesthesia of accessible mucous membrane of oral, larngyal and nasal cavities

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cocaine

Front 36

what local anesthetic that as the following?
se:
htn, tachycardia, arrhythmia

ci:
traumazied mucosa and sepsis

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cocaine

Front 37

used for the txmt of anxiety and ethanol dependence; also a primary agent in the txmt of status epilectus

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diazepam

Front 38

long acting,prototypic benzodiazepine binds to GABA-A receptor, increasing frequency of chloride channel opening

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diazepam

Front 39

used in txmt of parkinson disease, inhibits teh enzyme catechol-O-methyltransferase (COMT)

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entacapone

Front 40

inhibits the conversion of levadopa to 3-O-methyldopa in periphery, so inc dopa levels in the periphery and brain

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entacopone

Front 41

used as an adjunct for Sinement to reduce flucations, "off" time

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entacapone

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preferred agent in the txmt of absence seizures

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ethosuximide

Front 43

postulated to fxn by inhibiting T-type calcium channels in the thalamic neurons

-has been associated with the development of Steven-Johnson syndrome

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ethosuximide

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opioid used in the induction of anesthesia and also postoperative anlgesia

-used to tx moderate to severe pain, a potent analgesic

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fentanyl

Front 45

analgesic?

-duration of action : 30 to 60 min
-can produce bradycardia, treated with atropine
-may cause MUSCLE RIGIDITY esp respiratory muscles
-alters respiratory rate and alveolar ventilation -> may last longer than analgesic effect

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fentanyl

Front 46

analgesic contraindicated in pregnancy

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fentanyl

Front 47

analgesic which is drug of choice for pregnancy

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bupivacine

Front 48

popular drug used for txmt of depression, it is a prototype of selective serotonin reuptake inhibitors (SSRI)

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fluoxetine

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fluoxetine
sertraline
paroxetine
citalopram

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selective serotonin reuptake inhibitors (SSRI)

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ae:
-Headache
-insomnia
-nausea
-sexual dysfunction

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selective serotonin reuptake inhibitors (SSRI)

fluoxetine
sertraline
paroxetine
citalopram

Front 51

used to tx:
-depression
-obsessive compulsive disorder (OTC)
-social phobias
-bulimia
-alcohol dependence

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selective serotonin reuptake inhibitors (SSRI)

fluoxetine
sertraline
paroxetine
citalopram

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analog of GABA used in txmt of partial seizures, as well as in the managment of peripheral neuropathy

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gabapentin

Front 53

a neuroendocrine tumor of the medulla of the adrenal glands (originating in the chromaffin cells) or extra-adrenal chromaffin tissue which failed to involute after birth,[1] which secretes excessive amounts of catecholamines, usually epinephrine and norepinephrine.

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pheochromocytoma

Front 54

may cause life threatening Steven-Johnson syndrome and epidermal necrolysis

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gabapentin and lamotrigine

-both seizure medications

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seizure medication which inhibits GABA transaminases

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vigabatrin

Front 56

most potent inhaled halogenated anesthetic with lowest minimal alveolar concentration (MAC), used for surgical anesthesia in children and asthmatics

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Halothane

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se include:
-malignant hyperthermia
-fulminant hepititis in adults not children
-significant effects on cardiac rhythm

ci:
-do not give to pt with pheochromocytoma or OB pt

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halothane

Front 58

dissociative anesthetic that causes hallucination and disorientation on recovery

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ketamine

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moa: non-competitive antagonist of NMDA (N-methyl-O-aspartate)receptor, producing dissociative anesthesia
-analog of PCP

-used to induce and maintain general anethesia

Neuroprotective against:
-ischemic brain injury
-glutamate induced brain injury

ci: pregnancy

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ketamine

Front 60

anesthesic?
ae:
-hallucination or irriational behavior
-inc bp
-inc hr

-has a wide margin of safety

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ketamine

Front 61

used in txmt of parkinson disease, this precursor crosses the blood brain barrier and is converted to dopamine

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L-Dopa (levodopa)

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administered with decarboxylase inhibitor, carbidopa, which does not cross the bbb, to incr bioavailablity and to limit peripheral se

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L-dopa

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early se:
-anorexia, n/v, hypotension

late se:
-hallucination, delusion, agitation, insomina, patholgical gambling, hyper sexuality

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l-dopa

Front 64

mood stablizer that is a first line drug for txmt of bipolar affective disorder

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lithium

Front 65

inhibits 2nd messanger inositol triphosphase (IP3) and diacylglycerol (DAG) and causes tremor, hypothryroidism, polydipisa, and polyuria

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lithium

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amphetamine used in management of attention deficit disorder (ADD) and narcolepsy

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methylphenidate

Front 67

inc alertness and dec appetite by stimulating the release of catecholamines, a controlled substance with abuse potential

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methlphenidate

Front 68

inhaled anesthetic that never reaches the level of surgical anesthesia without addition of another agent, it is safe and teh induction and recover are extremely rapid

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Nitrous oxide

Front 69

moa: depresses excitatory N-methyl-D-Aspartate (NMDA)receptors

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nitrous oxide

Front 70

ae:
-degraded with vit B12 by intestinal bacteria - inactivation of methionine synthesis adn signs of vit B12 deficiency leading to megaloblastic anemia

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nitrous oxide

Front 71

-a non-halogenated general anesthetic

gas has high minimal alveolar concentraton (MAC) and a low blood/gas partition.

-usually is administered with an intravenous anesthetic such as thiopental, and is commonl used in dental procedures

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nitrous oxide

Front 72

older agent used in txmt of depression

-increases levels of amine neurotransmitters by inhibiting their breakdown

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Monoamine oxidase inhibitors (MAOI)

phenelzine
tranylcypromine
isocarboxazid

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what amino acid in foods such as cheese can react with MAOI to result in hypertensive crisis

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tyramine

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what other drug class if taken with MAOI cause serotonin syndrome?

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ssri - serotonin reuptake inibitors

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used as a sedative
-first line drug for tonic-clonic seizures in children
-used in txmt of pt with crigler-najjar syndrome type II

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phenobarbital

Front 76

long acting prototypic barbituate

moa: bind to GABA receptors increasing the duration of chloride channel opening with neuronal inhibition

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phenoparbital

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A potentially fatal drug interaction caused by combining drugs that raise the level of serotonin in the patient's nervous system to dangerously high levels. The symptoms of serotonin syndrome include shivering, overreactive reflexes, nausea, low-grade fever, sweating, delirium, mental confusion, and coma.

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serotonin syndrome

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An inherited defect in the ability to form bilirubin glucuronide, characterized by familial nonhemolytic jaundice and, in its severe form, by irreversible brain damage that resembles kernicterus.

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crigler-najjar syndrome

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drug used for txmt of partial and tonic-clonic seizures and status epilepticus, as well as being a class IB antiarrhythmic

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phenytoin

Front 80

anti-seizure and anti-arrhythmic drug that is a Na channel blocker

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phenytoind

other class IB anti-arrhythmics include:
1. lidocaine - acute txmt for ventricular arrhythmias
2. mexiletine
3. tocainide

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ae include:
-gingival hyperplasia
-hirsutism
-anemia
-birth defects, bc interferes with folate absorption

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phenytoin

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agent with largest number of extrapyramidal side effects of all atypical antipsychoitics

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risperidone

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atypical antipsychoitc with no extrapyramidal effects

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olanzpine

Front 84

group of drugs wich block D2 and h-HT2 receptors, contributing to high sedation

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atypial antipsychotics

including:
risperidone and olanzapine

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newly avaiable agent used in txmt of parkinson disease that forstalls the use of levodopa

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ropinirole

Front 86

non-ergot agent which acts on D2 receptors and is more effective than dopa with fewer se

-also used for restless leg syndrome

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ropinirole

Front 87

drug used to tx parkinson disease pt?

se:
-nausea
-hypotension
-pathologic gambling
-compulsion
-somnolence

Back 87

ropinirole

Front 88

2 non-ergot agets used to delay use of levodopa in parkinson pt

Back 88

ropinirole - act more on D2 recpetores
and
pramipexole - act more on D3 than D2 receptors

Front 89

inhibits the degeneration of dopamine in cns and is used as an adjuvant to levodopa in the txmt of parkinson disease

Back 89

selegiline

Front 90

inhibits monoamine oxidase B which selectively degrades dopamine

-irreversible MAO-B inhibitor
-acts within nerves

Back 90

selegiline

Front 91

ultra-short-acting bariturate used IV for induction of surgical anesthesia

Back 91

thiopental

Front 92

due to its high lipid solubility, this agent enters the cns within 1 min. can be used only for short surgical procedures bc it rapidly redistributes to other tissues

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thiopental

Front 93

slow injection recommended to minimize respiratory depression and possible overdose

-narrow window/margin btwn anesthetic effect and cardiovascular effect

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thiopental

Front 94

se of this antipsychotic includes torsade de pointes arrhythmias and retnal deposits

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thioridazine

Front 95

low potency antipsychotic blocks most dopamine receptors in cns and can cause postural hypotension, sedation and cns depression

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thioridazine

Front 96

used in txmt of most forms of epilepsy, including:
-generalized
-tonic-clonic
-partial absence
-myoclonic seizures
and
-in the txmt of bipolar disorders

Back 96

valproic acid

Front 97

anti-seizure meication?

moa:blocks Na and Ca channels

-associated with the development of neural tube defects in pregnant women

-must moniter liver fxn

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valproic acid

Front 98

drug is hightly effective in txmt of Absence Seizures due to it blocking effects on Ca channel

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valproic acid

Front 99

although not a benzodiazepine, it has similar effects and is used as a hypnotic with less dependence liablity

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zolpidem

Front 100

binds to benzodiazepine (BZD) receptors, has similar results as BZDs with less amnesia and less muscle muscle relaxation, also antagonized by flumazenil

Back 100

zolpidem