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105 Cards in this Set

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  • Back

Mechanismof action of nitroglycerin:

GTNis converted to nitric oxide.




NO isgenerated endogenously and acts as a vasodilator. It binds to guanylylcyclase and triggers a series of events that relaxes the vascular smoothmuscle.




Dilateslargecoronary arteries increasing oxygen supply to the heart muscle




Dilateslarge veins, reduces venous return to the heart , less blood to pump and lesswork load, less oxygen demand. –

Whydo we still use GTN?

Itisthe most effective agent acting acutely

Why treat hypertension?

•Untreatedleads to stroke, myocardial infarcts, vascular and kidney disease.

Antihypertensives

Any threeclasses of agents,but needto describe the consequencesofthe mechanisms.




Eg.Propranolol blocksbeta receptors in the heart. What doesthis do?

Why have antibiotic resistant organismemerged?

Reasons:


1) Overprescribing


2) Patientsdemand an antibiotic


3) SoldOTC in some countries


4) Nottaken properly by patient


5) Useof combinations


6) Inappropriateuse – not using sensitivity tests. 7) Prophylacticuse

Thegeneral population has a concept that herbals are non-toxic compared toprescription drugs. Why is this notcorrect?

Allsubstances can be toxic and toxicity should be determined on the basis of thesubstance and not on the source of the substance. A natural substance is the most toxicsubstance known to science.

•Designof a trial (Phase III)

–Whoand why?


–Randomassignment


–Doubleblind


–Objectivemeasures


–Stats

Factors affecting the concentration of the drug at the site of action

•Absorption


•Distribution


•Metabolism


•Excretion


•Knowdrug-interaction mechanisms

Themost common method by which drugs cross membranes is?

Simplediffusion through lipid

Theappearanceof a drug withdrawal syndrome signifies that the drug can produce:

Dependence

How does drug tolerance manifest?

It manifestsas a decrease in drug potency.

Thepropertythat makes benzodiazepines attractive as therapeutic agents is:

The widesafety margin (high therapeutic index).

On which receptor doesCannabis act?

CB1

What does Nitroglycerindo?

Nitroglycerindilates veins and reduces the return of blood to the heart.

VitaminC is required for?

VitaminC is required for the synthesis of collagen

The major mechanism of action of theestrogen/progestin oral contraceptive is?

Inhibition of ovulation.

The most effective contraceptive is?

Estrogen/progestinOC

Describe the mechanism of action for the following antibiotic/antifungal drugs:




1) Penicillin


2) Tetracycline


3) Sulfonamides


4) Itraconazole


5)Trimethoprim

1) Penicillin: inhibits cell wall synthesis




2) Tetracycline:Inhibits protein synthesis




3) Sulfonamides:Inhibits folate metabolism




4) Itraconazole:Inhibits cell membrane formation




5) Trimethoprim: Inhibits folate metabolism

Which mechanism lead to the therapeutic action of chlorpromazine (a phenothiazine) in schizophrenia?

Blockade of dopamine receptors

Tolerance occurs to which effects of the benzodiazepines?

Tolerance occurs to the SEDATIVE & HYPNOTIC effects of the benzodiazepines

The CNS depressant effects of ethanol are additive with ________?

Benzodiazepine

In the lungs, morphine causes?

Morphine – respiratory depression

Marijuana is classified by law as a ________?




And pharmacologically as a ___________?

as a narcotic




as a CNS depressant, euphoriant, hallucinogen

Pentazocine

= an opioid with mixed agonist/antagonist action

Zolpidem

= a new GABA receptor agonist which has minimal effects on sleep patterns

Flumazenil

= a GABA receptor antagonist




can be used as antidote for Benzodiazepine poisoning (Michael Jackson) (= a benzodiazepine receptor antagonist)

Phenobarbital

a narcotic and sedative barbiturate drug used chiefly to treat epilepsy.

Chronic ethanol abuse can result in ?

cirrhosis of the liver, an irreversible condition

Which mechanism leads to the therapeutic action of nifedipine in angina?

Blockade of calcium channels

Heparin mechanism of action

Heparin binds to antithrombin III, and enhances the action of antithrombin III

Low molecular weight heparins are _______ purified than heparin

Low molecular weight heparins are MORE purified than heparin

Mechanism of action of aspirin

?

For a young adult, normal blood pressure is?




The higher figure is?


The lower figure is?

For a young adult, normal blood pressure is about 120/80;




the higher figure is the systolic and the lower figure the diastolic blood pressure

define systolic & diastolic

systolic = when heart is contracting




diastolic = when heart is in between contractions

The definition of normal blood pressure depends on ?

The definition of normal blood pressure depends on the age of the individual, with the normal value in creasing with age

Hydrochlorothiazide mechanism of action

Hydrochlorothiazide decreases the volume of fluid in blood vessels by enhancing sodium and water excretion

Clonidine mechanism of action

?

Mechanism of action of lovastatin (a statin)

Inhibition of the rate-controlling enzyme in cholesterol (!) synthesis

Which mechanism leads to the therapeutic action of propranolol in angina?

Blockade of beta receptors

The lipoprotein referred to as the “bad” lipoprotein is:

LDL

Warfarin mechanism of action

Warfarin acts as a vitamin K antagonist




---> inhibits the synthesis of clotting cofactors

Tissue plasminogen mechanism of action

?

Which of the penicillins is resistant to the action of penicillinase?

Methicillin

Which of the following is the target for the bactericidal action of penicillin G?

Cell walls




penicillin G = natural penicillin

Antivirals for Influenza:

Amantidine and Oseltamivir (Tamiflu)




Oseltamivir inhibits the enzyme that allows for the spread of the virus

In 1961 in England an epidemic resulted in the death of young turkeys, ducks and chickens.


---> attributable to the peanut meal used as poultry feed. The peanuts were contaminated with the fungus "Aspergillus flavus" which produced the carcinogen, ___________(1).


Which kind of cancer was induced this carcinogen (2)?

1) aflatoxin


2) liver cancer

Which of the modifiable, environmental factors cause the most cancer deaths?

Tobacco and nutrition

An anticancer drug that blocks estrogen from binding to its receptor is best-described as:

Hormone antagonist

The cancer anticipated to lead to the largest number of deaths in Canada is:

lung cancer

Co-trimoxazole is a combination of trimethoprim and:

Sulfamethoxazole

Augmentin is a combination of amoxacillin and:

Clavulinic acid

Toxicity associated with sodium benzoate?

There is no real known toxicity associated with sodium benzoate as it is rapidly metabolized and excreted in humans.

Smoke is both a food preservative and ?

and flavouring agent

Sodium chloride

one of the first compounds used as a preservative

Toxicity associated with Texture Agents?

Texture agents possess little or no toxicity.

Gossypol:

Potential Male Contraceptives




obtained from cottonseed




destroys elements of the seminiferous tubules, decreasing sperm production




recovery of sperm count after discontinuing use of gossypol is not always guaranteed




led to a reduction in sperm count in 99% of the subjects.

simulated flavours

simulated flavours are mixtures of artificial flavours.

monosodium glutamate (MSG)

MSG causes a tightening of muscles in the face and neck, accompanied by headache.




= a flavour enhancer

Drug use by athletes to




1) Increase endurance and speed


2) Increase strength.


3) Reduce body weight.

1) amphetamines (often results in less than 5% increase in athletic performance)




2) Anabolic steroids & growth hormone




3) Diuretics to reduce body water, and thus weight

Mifepristone (RU-486)

Mifepristone (RU-486) is an anti-progestin and is taken after a “missed period”

Food additives

substances added to food to improve appearance, texture, storage, and nutritional value of food

effective cough suppressants (antitussives)

Codeine and dextromethorphan HBr

Which vitamin requires successive biotransformation (chemical change) in the liver AND kidney to become a biologically active substance?

Vitamin D

Arguments (circumstantial evidence) for the dopamine hypothesis of schizophrenia

1) binding affinity of drug to the receptor is highly correlated with their antipsychotic potency




2) drugs that increase dopamine aggravate/induce schizophrenia




3) dopamine receptor density is increased in (untreated) schizophrenics (compared to non-schizophrenics)



3 features of 2nd generation antipsychotics

1) treat positive AND negative symptoms




2) less extrapyramidal side effects




3) block both dopamine AND serotonin receptors

Drugs for bipolar disorder

lithium carbonate (mood stabilizer, many adverse effects)




anticonvulsants




(plus antidepressants and antipsychotics for depressive and manic phase)



phenobarbital was the first _____________ while chlordiazepoxide was the first _____________

phenobarbital was the first barbiturate while chlordiazepoxide was the first benzodiazepine

mechanism of action of barbiturates & benzodiazepines

reduce glutamate-induced excitation (anxiety) by enhancing GABA inhibition

Barbiturates _________ REM sleep, while benzodiazepines ___________, and the drug Zolpidem __________

Barbiturates suppress REM sleep, while benzodiazepines do so less, and the drug Zolpidem even less

what benzodiazepine is drug of choice for panic disorder?

Alprazolam

Buspirone

anti anxiety drug (acts on serotonin receptor)




advantage: no additive effects with other sedative-hypnotic drugs

Gamma-hydroxybutyric acid (GHB)

= date rape drug




GABA agonist

diazepam

anticonvulsant (against seizures)




can treat alcohol withdrawal (cross-dependance principle)

major site of absorption of alcohol

upper small intestine

alcohol distributes via the ____________?

total body water

how much pure alcohol is metabolized in 1 hour?

13 ml

drugs to treat alcohol abuse act by _______?

they inhibit ADH, which leads to the accumulation of acetaldehyde --> making person feel ill




(i.e. disulfiram)

a person twice as likely to have an accident, has a blood alcohol level of ______?

0.05%


50mg/100ml






(with 0.08% the chance are 8 (!) times higher)

effects of chronic high use of alcohol

1) CNS: damages axons --> alcoholic dementia




2) Cardiovascular: alcoholic cardiomyopathy (destruction of heart muscle), hypertension, stroke




3) Liver: alcoholic liver disease




4) Vitamin B1: thiamine deficiency (results ion Wernicke & Korsakoff syndromes)




5) Peripheral NS: damages axons (loss of feeling in feet, pain, difficulty walking)

3 stages of alcoholic liver disease

fatty liver (reversible) ---> alcohol hepatitis (usually reversible) ---> cirrhosis (not reversible)






alcohol hepatitis = inflamed liver


cirrhosis = scar tissue on liver, impairing blood flow

Alcohol withdrawal produces _______________ of the CNS

excitability




(restlessness, anxiety, sweating)

delirium tremens

= a severe alcohol withdrawal symtom




1) tremolousness


2) hallucinations


3) confusion


4) psychomotor agitation


5) sleep disorders




starts later (3rd day of disuse) and lasts longer than other symptoms

drugs used in treatment of alcoholism

1) disulfiram (--> person feels ill)




2) naltrexone (diminishes craving)




3) acomprosate (ethanol subsitute) (evidence is not overwhelming)

What is the endogenous ligand for cannabis receptors?

Anandamide, a retrograde transmitter (post to presynaptic neuron)




when receptor gets activated: inhibits release of excitatory neurotransmitters

treat alcohol dependance with ___________ and opioid dependance with ____________

alcohol: naltrexone




opioids: naloxone

heroin is more ________ then morphine, but not more __________

heroin is more potent then morphine, but not more efficacious

rickets

vitamin D

scurvy

vitamin C

beriberi

vitamin B1 (thiamin)

pellagra

vitamin B3 (niacin)

pernicious anemia

vitamin B12

1) Alzheimers: loss of _______ neurons from ________




2) Parkinson's: loss of _______ neurons from ________




3) Huntington's: loss of neurons from the ________

1) cholinergic, cortex




2) dopaminergic, substantia nigra




3) striatum

1) which class of drugs produces no dependence?




2) and which produces no tolerance?

1) hallucinogens




2) nicotine

sympathetic

fight and flight

parasympathetic

rest and relax

peripheral NS

somatic - voluntary




autonomic - involuntary:


-sympathetic & parasympathetic

Lou Gehrig's disease (ALS): loss of neurons in __________

spinal cord & brain

cocaine inhibits reuptake of





dopamine & norepinephrine

cocaine abuse liability & inherent harmfulness =

highest among all abused drugs

caffeine mechanism of action

block ADENOSINE receptors, which ?????

when body contains alcohol it ______ biotransformation, when body contains no alcohol it ______ biotransformation

1) decreases




2) increases

which 2 vitamins are antioxidants?

vitamin C and E

which vitamin is involved in homocysteine levels?

vitamin B6

which vitamin is involved in night vision?

vitamin A

which vitamin causes rickets & osteoporosis ?

vitamin D