All antipsychotic agents are ________ at D2 dopamine receptors.

antagonists

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

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

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

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

&

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

What is the current anorexiant of choice?

Sibutramine

- blocks reuptake of NorEpi and 5HT

- does not cause 5 HT (serotonin) release

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

A. Phenytoin

B. Carbamazapine

C. Clonazepam

D. Clorazepate

C. Clonazepam

- generalized seizures include:

Absence (petit mal)

Myoclonic

Tonic-Clonic (grand mal)

Tonic

Clonic

Atonic

Status epilepticus

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

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)

Which is not an adverse affect of Phenytoin?

A. osteomalacia

B. gingival overgrowth

C. rickets

D. ataxia

E. nystagmus

F. pancreatitis

G. cardiovascular collapse

F. pancreatitis

- this is associated with carboxylic acid (valproic acid)

What affect do benzodiazepines have on stage 2 sleep?

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

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

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

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

A. Directly bind GABA_A receptors

B. Directly bind GABA_B receptors

C. Directly bind GABA transporters

D. Directly bind near GABA_A receptors

D. Directly bind near GABA_A 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.

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

A. Alzapam/Lorazepam

&

D. Serax/Oxazepam

- both drugs are slowly absorbed and rapidly eliminated

Which of the following is a BZ1 receptor antagonist?

What is it used for?

A. Eszopiclone

B. Flumazenil

C. Zolpidem

D. Zaleplon

B. Flumazenil

- used for benzodiazepine overdose

- given by IV, short half-life

- side effects: dizziness, agitation, confusion, nausea

Which novel benzodiazepine can be safely presribed to pregnant women?

Zolpidem (Ambien)

- decreases sleep latency

- minimal muscle relaxant and anticonvulsant effects

- antagonized by Flumazenil

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

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

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

Quazepam (Doral)

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

A. Chloral hydrate

B. Hydroxyzine

C. Buspirone

D. Thiopental

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

What type of drug is Fluoxetine?

What is its trade name?

What is it used to treat?

Fluoxetine = Prozac = SSRI

- used to treat depression

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

- low fatality

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

What is their molecular action?

What do they treat?

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)

What is serotonin syndrome?

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

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

Pramipexole

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

- increased efficacy and fewer psychotic effects than ergot-alkaloids

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

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

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

D. Vincristine

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

E. Doxorubicin

- generates free-radicals, linked to heart complications

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

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)

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?

L-dopa

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

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

D. all of the above

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

- has bad interactions with tricyclins and serotonin reuptake inhibitors

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?

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)

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

Minimum Alveolar Concentration

 - Also equivalent to the ED50

- determined by lipid/gas solubility coefficient

- working range .8 to 1.2

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

A. Potent Analgesic

D. Weak Anesthetic

F. Low lipid solubility

- can cause diffusion hypoxia during recovery

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

Dantrolene

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

Enflurane

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

A. Halothane

B. Enflurane

C. Isoflurane

D. Desflurane

D. Desflurane

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

Isoflurane

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

Succinylcholine

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?

Absence

Ethosuximide

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

Carbamazepine

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

inhibitory = GABA

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

Vigabatrin - inhibits GABA transaminase (increases intracellular GABA)

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?

Tranylcypromine

- an MAO inhibitor

- has toxic interactions with foods rich in tyramine

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

insulin - lispro

- ultra short-acting

- insulin glargine controls fasting glucose

Which does not decrease insulin requirements?

A. Corticosteroids

B. Beta blockers

C. Alcohol

D. Oral Hypoglycemics

A. Corticosteroids

- they increase insulin requirements

- so do oral contraceptives

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?

Glyburide - for fasting

Repaglinide - for postprandial

*both cause weight gain

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

Clozapine