Dr. Deb exam 2 multiple choice

The drug 2-PAM is used as an ______________ to poisoning with _____________ inhibitors.

Antidote, Cholinisterase

What is an ideal mutual prodrug? Give two examples.

Aspirin, paracetamol

L-DOPA stands for ______________.

L-3-dihydroxyphenylalanine

A sentry drug is a drug that is taken to ____________ another drug from undesired ______________ action.

Protect, enzymatic

"Bystander effect" is observed in ____________.

Suicide Enzyme prodrug therapy

The abbreviation ADMET stands for _________.

Absorption distribution metabolism excretion toxicity

What is 'serotonin syndrome?

A life threatening drug reaction that causes the body to have too much serotonin

Cell membrane is permeable to many drug molecules but not to others, depending on their ____________ solubility.

Lipid

Small pores, ___________ angstroms, permit small molecules such as alcohol and water to pass through.

8

Bound drugs are _____________ inactive because the drug-protein complex is unable to cross cell membranes.

Pharmacologically

The ____________ of metabolism of a drug determines the duration of the action of the

drug.

Rate

In general, the __________ of a drug occurs after a drug has been given for approximately ___________ elimination half-lives.

Steady state, 5

Sulindac is a prodrug for _____________ sulfide, the metabolite reductive product

Sulindac

N-oxidation prodrug activation reaction is reversible ____________ drug delivery strategy for getting drugs into the ____________

Redox, brain

'Absorption' is the process of drug _________ from the administration site to the systemic ____________.

Movement, circulation

Drug absorption is mainly in the upper __________ that is facilitated by the large surface area of ___________ and the rich blood supply.

Small intestine, Villi

If two drugs are administered concurrently, the drug with the __________ affinity will be preferentially bound and displace the drug with the __________ affability from the protein binding site.

Higher, lower

Vd < 0.071 L/kg indicate the drug is mainly in the ____________ system whereas Vd > 0.071 L/kg indicate the drug has entered in the specific ___________.

Circulatory, tissues

Clearance is a ___________ and determines the ____________ dose.

Constant, maintenance

Volume of __________ gives information on how the drug is distributed in the body.

Distribution

Volume of distribution is a theoretical Volume and determines the _________ dose

whereas clearance is a constant and determines the _________ dose

Loading, maintenance

Drugs are metabolized in the liver, lungs, kidneys, blood and ____________.

Intestines

Drugs are primarily excreted by the _____________ and it can be affected by the urinary ___________.

Kidneys, pH

The half-life of a drug is the time required for the concentration of the drug in the __________ to decrease by one-half of its __________ value.

Plasma, intitial

In theory, the optimal dosage interval between drug ___________ is equal to the ___________ of the drug

Administration, half-life

Diethylstilboestrol is a drug for ____________ carcinoma.

Prostatic

Why methenamine is used as a urinary tract antiseptic instead of formaldehyde?

Formaldehyde is more toxic than methenamine

Candoxatril is a prodrug for chronic heart failure where 5-indanol group serves the role of a __________________ group.

Electron withdrawing

Write the common name & chemical structure of important neurotransmitters.

Glycine = G

Alanine = A

Valine = V

Leucine = L

Proline = P

The common name of (I) is __________ which is an important neurotransmitter.

Isoleucine

In general, the ________ of amines can be lowered by __________ units by conversion to N- Mannick bases.

pka , 3

Imines, oximes, ketals, ________ and __________ are masked carbonyl compounds.

Oxazolidine, Thizolidine

To increase the water solubility of _________ (anticancer, topoisomerase inhibitor), it has been converted to the _________ prodrug.

Etoposide, phophate

Carrier-linked prodrugs largely use __________ activation

Hydrolytic

___________ prodrugs mostly use oxidative or reductive activation

Bioprecursor

The metabolically-activated ____________ agents are actually examples of __________ prodrugs.

Alkylating, bioprecursor

Bioprecursor prodrugs can be activated by oxidation, ___________ or ______________.

Reduction, phosphorylation

The ____________ are a family of ____________ -containing natural products isolated from Streptomyces caespitosus or Streptomyces lavendulae

Mytomycins, aziridine

The anti-arthritis drug sulindac is an ____________ isostere of indomethacin, which originally was designed as a _______________ analog.

Indene , serotonin

Demethylation is a ___________ type of reaction whereas Sulfate conjugation is a ______________ type of reaction.

Phase 1, phase 2

The ____________ is the fraction of drug in the body which is removed per unit time.

Elimination rate constant

At steady-state the rate of drug ___________ equals the rate of _____________ and plasma ______________.

Administration, elimination, concentration

In P450 interactions, inducer stands for a specific drug that enhances a specific hepatic ____________

Isozyme

Drugs with high lipid _____________ are reabsorbed passively and therefore slowly _____________

Solubility, excreted

Pharmacodynamics of a drug depends on receptors, ______________ enzymes, ______________ and chemotherapy.

Ion channels, carrier molecules

G-protein-couple receptors can work in _____________.

Seconds

Calcium channel blockers prevent _____________ of calcium through the cell membrane.

diffusion

Carrier molecules allow transport of small organic molecules that are too ___________ not sufficiently ___________ soluble to penetrate cell membranes on their own.

Polar, lipid

P450 activity is ___ determined?

Generally

The % of the bound drug is a ratio of ____________ drug and a combination (summation) of bound drug and ____________ drug.

Bound, free

The term "abzyme" indicates a combination of ____________ and ______________.

Antibody, enzyme

___________ and ____________ are two examples of carrier molecules

Nicotinamine adenine dinucleotide, Coezyme Q

_____________ is a precursor or building block to _____________, which lead to inflammation and escalate the sensation of pain.

Arachidonic acid, Prostaglandins

________________ enzymes convert arachidonic acid to prostaglandins.

Phospholypase A2

All non-steroidal anti-inflammatory drugs inhibit ____________ enzymes.

Cyclooxygenase (COX)

Arachidonic acid is a polyunsaturated ____________ with a 20-carbon chain and four ___________ bonds.

Fatty acid, double

Every ____________ contains 20 carbon atoms, including a _____________ carbocyclic ring.

Fatty acid, three member

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