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Pharmacology
3rd test
43
Pharmacology
Professional
04/29/2010

Additional Pharmacology Flashcards

 


 

Cards

Term

 

All antipsychotic agents are ________ at D2 dopamine receptors.

Definition

 

antagonists

Term

 

Which is more likely to cause tardive dyskinesia: atypical or typical antipsychotics?

Definition

 

typical

 

- tardive dyskinesia is characterized by involuntary repetetive movements, can be side effect of long-term or high dose typical antipsychotics

- newer, atypical drugs better at reducing this

Term

 

Partial agonists might be considered ideal drugs for schizophrenia because they act as ________ in the _________ pathway, and as _________ in the ____________ pathway.

Definition

 

they act as functional antagonist in the mesolimbic pathway, improving positive symptoms

&

they act as functional agonist in the mesocortical pathway, improving negative symptoms

Term

 

What is the current anorexiant of choice?

Definition

 

Sibutramine

 

 

- blocks reuptake of NorEpi and 5HT

- does not cause 5 HT (serotonin) release

Term

 

Which of the following drugs is used to treat primarily generalized seizures?

 

A. Phenytoin

B. Carbamazapine

C. Clonazepam

D. Clorazepate

Definition

C. Clonazepam

 

- generalized seizures include:

Absence (petit mal)

Myoclonic

Tonic-Clonic (grand mal)

Tonic

Clonic

Atonic

Status epilepticus

 

Term

 

Anticonvulsants exert their effects through GABA and glutamate receptors, and through ion channels. Where do Phenytoin, Carbamazepine, and Valproic Acid exert their effects?

 

 

Definition

 

They all inhibit voltage-gated Na+ channels. This prevents the cell from depolarizing, which prevents the release of glutamate from the pre-synaptic terminal.

 

- they bind Na+ channels in inactive state, prolonging inactivation (use-dependent block)

 

Term

Which is not an adverse affect of Phenytoin?

 

A. osteomalacia

B. gingival overgrowth

C. rickets

D. ataxia

E. nystagmus

F. pancreatitis

G. cardiovascular collapse

 

Definition

 

F. pancreatitis

 

 

- this is associated with carboxylic acid (valproic acid)

 

 

Term

 

What affect do benzodiazepines have on stage 2 sleep?

Definition

 

They increase its duration

 

(stage 2 is non-REM)

 

- Sleep onset time, duration of REM sleep, and stage 4 non-REM slow wave sleep are all decreased with benzodiazepines

Term

 

CNS depressants have an ________ effect. Low doses cause ________, while high doses cause _________.

Definition

 

CNS depressants have an additive effect. Low doses cause anxiolysis , while high doses cause coma/death.

Term

How do Alprazolam, diazepam, oxazepam and triazolam exert their molecular effect?

 

A. Directly bind GABAA receptors

B. Directly bind GABAB receptors

C. Directly bind GABA transporters

D. Directly bind near GABAA receptors

Definition

 

D. Directly bind near GABAA receptors


 

Benzodiazepines by themselves do not open GABAA channels- instead they enhance the ability of GABA to open GABAA channels, increasing frequency of opening when GABA is present.

 


Term

 

Which of the following benzodiazepines would be used to treat anxiety in a patient with liver disease?

 

A. Alzapam/Lorazepam

B. Xanax/Alprazolam

C. Valium/Diazepam

D. Serax/Oxazepam

Definition

 

A. Alzapam/Lorazepam

&

D. Serax/Oxazepam

 

 

- both drugs are slowly absorbed and rapidly eliminated

Term

 

Which of the following is a BZ1 receptor antagonist?

What is it used for?

 

A. Eszopiclone

B. Flumazenil

C. Zolpidem

D. Zaleplon

Definition

 

B. Flumazenil

 

 

 

- used for benzodiazepine overdose

- given by IV, short half-life

- side effects: dizziness, agitation, confusion, nausea

Term

 

Which novel benzodiazepine can be safely presribed to pregnant women?

Definition

 

Zolpidem (Ambien)

 

- decreases sleep latency

- minimal muscle relaxant and anticonvulsant effects

- antagonized by Flumazenil

Term

Match each of the following specific properties to benzodiazepines or barbituates:

 

A. Most metabolites lack pharmacological activity

B. Overdose can be treated with Flumazenil

C. High therapeutic index, wide margin of safety

D. Are GABA-mimetic at high concentrations

Definition

A. Most metabolites lack pharmacological activity:

Barbituates

B. Overdose can be treated with Flumazenil:

Benzodiazepines

C. High therapeutic index, wide margin of safety:

Benzodiazepines

D. Are GABA-mimetic at high concentrations:

Barbituates

Term

 

Which Benzodiazepine sedative-hyponotic is selective for BZ1 receptors, and so is less likely to cause drug tolerance and muscle relaxation in the patient?

Definition

 

Quazepam (Doral)

Term

 

Which of the following anti-anxiety/sedatives do NOT bind the GABA receptor complex?

 

A. Chloral hydrate

B. Hydroxyzine

C. Buspirone

D. Thiopental

Definition

B. Hydroxyzine

&

C. Buspirone

 

- hydroxyzine is an H1 histamine receptor antagonist

- buspirone is a 5HT1A serotonin receptor partial agonist and a mixed antagonist/agonist at dopamine receptors

Term

 

What type of drug is Fluoxetine?

What is its trade name?

What is it used to treat?

Definition

 

Fluoxetine = Prozac = SSRI

 

- used to treat depression

(also panic disorder, OCD, ADD, chronic pain, bulimia)

- low fatality

Term

 

Phenelzine, Tranylcypromine, and Moclobemide are all what type of drug?

 

What is their molecular action?

 

What do they treat?

Definition

All MAO inhibitors

 

-Moclobemide is selective for monoamine oxidase type A

(metabolizes tyramine, norepi, and serotonin)

-Other two bind and block types A and B

(MAO type B metabolizes dopamine)

 

Used to treat depression

(also panic disorder, OCD, ADD, chronic pain, bulimia)

Term

 

What is serotonin syndrome?

Definition

 

A dangerous interaction between SSRIs and MAO inhibitors. Too much serotonin (not being broken down) results in hyperthermia, muscle rigidity, myoclonus, alteration of vital signs and mental status, anxiety, insomnia, rashes, decreased libido, sexual dysfunction.

 

- can be lethal

 

Term

 

Which non-ergot alkaloid can be used as a monotherapy to treat late-stage Parkinson's?

Definition

 

Pramipexole

 

- Preferentially binds D3 receptors, also D2 & D4, not D1

- increased efficacy and fewer psychotic effects than ergot-alkaloids

Term

 

What long-time cancer therapeutic is primarily a thymidilate synthase inhibitor?

Definition

 

5-FU (fluorouracil)

 

- pyrimidine analog

- actively transported into the cell & converted to corresponding nucleotide (resistance can develop here)

- blocks thymidine synthesis --> affects DNA & RNA synthesis

 

 

Term

 

Which of the following chemotherapeutic agents bind to tubulin, inhibiting microtubule formation, and hence mitosis?

 

A. Cyclophosphamide

B. Gleevec

C. 6-Mercaptopurine

D. Vincristine

E. Doxorubicin

Definition

 

D. Vincristine

Term

Which of the following chemotherapeutic agents interacts with DNA through intercalation and prevents resealing of the DNA chain through interaction with topoisomerase II, thus stopping replication and biosynthesis?

 

A. Cyclophosphamide

B. Gleevec

C. 6-Mercaptopurine

D. Vincristine

E. Doxorubicin

Definition

 

E. Doxorubicin

 

 

- generates free-radicals, linked to heart complications

Term

 

Which hypoglycemic drug could you prescribe to a diabetic patient to help them control blood sugar and lose weight?

 

A. Sulfonylureas (Glyburide, Micronase, Glynase)

B. Meglitinides (Repaglinide, Prandin)

C. Pramlintide

D. Exenatide

Definition

C. Pramlintide

or

D. Exenatide

 

- both are injected, decrease gastic emptying

- Pramlintide can be used alone w/ insulin or in combo with metformin and/or sulfonylrureas

- Exenatide also monotherapy or in combination, contraindicated in renal disease

- (Sulfonylureas and Meglitinides cause weight gain)

 

 

 

Term

 

What intermediate stage therapy for Parkinson's has adverse side effects that include AIM/rigidity (on-off phenomena), orthostatic hypotension, nausea, vomiting, CV effects, and adverse mental effects?

Definition

 

 

L-dopa

 

- patient should restrict B6 in diet to help minimize peripheral metabolism by AAAD

Term

 

Selegiline, an MAO-B selective early stage Parkinson's therapeutic, should not be administered with which of the following?

 

A. L-dopa

B. Tricyclics

C. serotonin reuptake inhibitors

D. all of the above

Definition

D. all of the above

 

 

- if administered with L-dopa, can result in hypertensive crisis

- has bad interactions with tricyclins and serotonin reuptake inhibitors

Term

 

Which drug can be given along with L-dopa in intermediate stage Parkinson's therapy to reduce peripheral metabolism of L-dopa by AAAD?

 

Metabolism by COMT?

Definition

 

Carbidopa prevents peripheral metabolism by AAAD

(B6 restriction helps)

 

Tolcapone acts both centrally and peripherally to restrict metabolism by COMT

(can cause diarrhea, increase L-dopa adverse affects)

Term

 

______ is the partial pressure of an inhaled anesthetic which when breathed for 15 min produces surgical anesthesia in 50% of the population.

Definition

 

Minimum Alveolar Concentration

 

 

 - Also equivalent to the ED50

- determined by lipid/gas solubility coefficient

- working range .8 to 1.2

Term

 

Which is true of N20?

 

A. Potent Analgesic

B. Potent Anesthetic

C. Weak Analgesic

D. Weak Anesthetic

E. High lipid solubility

F. Low lipid solubility

Definition

 

A. Potent Analgesic

D. Weak Anesthetic

F. Low lipid solubility

 

- can cause diffusion hypoxia during recovery

Term

 

Malignant hyperthermia can occur with inhalation anesthetics. What drug is used to counter act this?

Definition

 

 

Dantrolene

Term

 

This inhalation anesthetic is similar to halothane in effects, but is less likely to induce cardiac arrythmias, and is contraindicated for epileptic patients.

Definition

 

 

Enflurane

Term

 

Malignant hyperthermia has not been reported in which of the following inhalation anesthetics?

 

A. Halothane

B. Enflurane

C. Isoflurane

D. Desflurane

Definition

 

D. Desflurane

 

 

 

Term

 

This inhalation anesthetic is less blood soluble than Enflurane, more irritating to respiratory tract, and can dilate coronary arteries leading to coronary "steal".

Definition

 

Isoflurane

Term

 

Chest wall spasm resulting from Innovar (neuroleptic-opioid combination) can be treated with ________.

Definition

 

Succinylcholine

Term

 

What type of generalized seizure is common in childhood?

 

A. Absence

B. Myoclonic

C. Atonic

D. Reflex

 

What is the treatment of choice for it?

Definition

 

 

Absence

 

Ethosuximide

Term

 

Which anticonvulsant am I?

 

-I reduce my own half-life and those of other drugs through low protein binding & activation of CYP3A4

- I exacerbate absence and myoclonic seizures, though I'm good at treating tonic-clonic and partial seizures

- CYP3A4 inhibitors, like erythromycin, increase my plasma levels

Definition

 

Carbamazepine

Term

 

The anticonvulsants Tiagabine and Vigabatrin both have their molecular action on inhibitory neurotransmission. What are their molecular targets?

Definition

 

inhibitory = GABA


Tiagabine - inhibits GABA transporter so it remains in synaptic cleft longer

Vigabatrin - inhibits GABA transaminase (increases intracellular GABA)

 

 

 

Term

 

A patient is taking an anti-depressant. Their doctor tells them not to eat a lot of cheese or other fermented foods.

Which antidepressant are they likely taking?

Definition

 

Tranylcypromine

 

- an MAO inhibitor

- has toxic interactions with foods rich in tyramine

Term

 

What would you inject into a diabetic to control their postprandial glucose level?

Definition

 

insulin - lispro

 

- ultra short-acting

 

- insulin glargine controls fasting glucose

Term

 

Which does not decrease insulin requirements?

 

A. Corticosteroids

B. Beta blockers

C. Alcohol

D. Oral Hypoglycemics

Definition

 

A. Corticosteroids

 

- they increase insulin requirements

- so do oral contraceptives

Term

 

Glyburide (a Sulfonurea) and Repaglinide (a Meglitinide) both act as insulin secretagogues through inhibition of ATP-sensitive K+ channels. Which one is indicated for control of fasting glucose, and which is used for postprandial?

 

 

Definition

 

Glyburide - for fasting

 

Repaglinide - for postprandial

 

 

*both cause weight gain

Term

 

Agranulocytosis can be caused by what antipsychotic drug that's used to treat schizophrenia?

Definition

 

 

Clozapine

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