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Organic Medicinal Chemistry > Objective Information > Flashcards

Objective Information Flashcards

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1
Q

A modified bacterial form that has been made nontoxic but remains the ability to stimulate the formation of antitoxin.

A

Toxoid

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2
Q

A product derived from blood plasma of a donor pool similar to the IG pool but prepared so it is suitable for IV use. Indications: Ab deficiency & Kawasaki’s disease.

A

Intravenous Immune Globulin (IVIG)

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3
Q

A type of immunobiological that contains a solution of antibodies derived from the serum of animals immunized with specific antigens.

A

Antitoxin

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4
Q

A genetically engineed chimeric monoclonal antibody directed against CD20 antigen on malignant B lymphocytes.

A

Rituximab

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5
Q

A monoclonal antibody approved for breast cancer which selectively binds with high affinity to the extracellular domain of human epidermal growth factor 2 protein.

A

Transtuzumab

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6
Q

It is also known as Interluekin-2 or T-cell growth factor. This product when administtered stimulates T-cell growth and regulation, proliferation, and immunoglobulin production in B lymphocytes and macrophage activity enhancement.

A

Aldesleukin

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7
Q

A highly purified protein produced by E.coli containing a plasmid with an alfa-2b gene. This product is indicated for hairy cell luekemia and also useful in treating malignant melanoma.

A

Interon

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8
Q

A highly purified protein manufactured from a strain of E. coli bearing a genetically engineered plasmid containing an interferon alfa-2a gene from human leukocytes. Indication: hairy cell luekemia and chronic myelogenous leukemia (18 y/o and above).

A

Roferon-A

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9
Q

The only insulin analogue with a C14 fatty acid attached to an amino acid residue in the B chain of insulin.

A

Detemir

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10
Q

Drug with a strong structural relationship to the meperidine-type analgesics and has the ability to inhibit excessive GI motility.

A

Diphenoxylate

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11
Q

A.k.a. N-cyclobutylmethylnoroxymorphone hydrochloride. An analgesic of the agonist-antagonist type with little or no abuse liability.

A

Nalbuphine

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12
Q

Drug prepared by N-demethylation of morphine and has 1/4 activity as morphine but has much lower physical dependence capacity.

A

Normorphine

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13
Q

Drug which has a fragment of codeine’s structure. Has opioid activity but has other analgesic activity not reversed by naloxone.

A

Tramadol HCl

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14
Q

Analgesic 2-3x more potent than morphine.

A.k.a. heroin.

A

Diacetylmorphine HCl

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15
Q

Aromatase Inhibitor used mainly for Cushing’s syndrome.

A

Aminoglutethimide

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16
Q

Which of these drugs is NOT a nonsteroidal aromatase inhibitor?

a. Letrozole
b. Aminoglutethimide
c. Exemestane

A

Exemestane

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17
Q

Anti-estrogen which is an antagonist structurally based on the estradiol structure which is used in the tx of women who have had disease progression after prior antiestrogen therapy.

A

Fulvestrant

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18
Q

SERM which is a benzothiophene derivative.
Indication: osteoporosis in menopausal women.
Has antagonist properties on the endometrium and breast tissue and agonist properties on bone and the cardiovascular system.

A

Raloxifene

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19
Q

SERM which has a triphenylethylene structure used to treat early and advanced breast carcinoma in postmenopausal women.

A

Tamoxifen

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20
Q

S-adenosylmethionine is required for this conjugation reaction.

A

Methylation

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21
Q

This conjugation pathway is extremely important in preventing toxicity from a variety of electrophilic agents. It produces a mercaptopuric acid derivative upon reaction with an electrophile.

A

Glutathione conjugation

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22
Q

Buspirone is an anxiolytic agents that is a partial agonist to ___ receptor.

A

5HT1A

23
Q

Sumatriptan and other indolealkylamine derivatives used in the treatment of migrane is an agonist at ___ receptor.

A

5HT1D

24
Q

It is an isoquinoline derivative with most of the biological activity found in the levo enantiomer. The comound has no activity against nematodes, but is highly effective against cestodes and trematodes.
MOA: Ca ion redistribution and inhibition of phosphoinositide metabolism.

A

Praziquantel

25
Q 
A drug that belongs to a class of 16-membered macrocyclic lactones extracted from S.avermitilis.
Indication: various nematode infections.
MOA: GABA agonist and inducer of Cl ion influx leading to hyperpolarization and muscle paralysis.
A

Ivermectin

26
Q

A drug that acts as a depolarizing neuromuscular blocking agent that activates nicotinic receptors and inhibits cholinesterase leading to worm paralysis.
Available as a pamoate salt. Not readily absorbed thus improving is usefulness against intestinal helminths.

A

Pyrantel

27
Q

Drug which has been highly effective againts Schistosoma mansoni. It is activated via esterification to a biological ester that spontaneously dissociates to an electrophile, which alkylates the helminth DNA, leading to irreversible inhibition of nucleic acid metabolism.

A

Oxamniquine

28
Q

1st generation sulfonylureas (3)

A

Chlorpropamide
Acetohexamide
Tolbutamide

29
Q

2nd generation sulfonylureas (3)

A

Glyburide
Glipizide
Glimepiride

30
Q

Prodrug designed to prolong drug activity.

A

Azathioprine (converted to 6-mercaptopurine)

31
Q

Prodrugs designed to mask drug toxicity and side effects.

A

Aspirin (converted to salicylic acid)
Cyclophosphamide
Aciclovir & Penciclovir

32
Q

Prodrug designed to lower water solubility.

Mask bitter taste

A

Chloramphenicol palmitate

33
Q

Prodrug designed to increase water solubility.

For IV drugs to get higher concentration and decrease pain from low solubility at the injection site.

A

Chloramphenicol succinate

34
Q

Prodrug used in the targeting of drugs (e.g. released at specific sites under specific conditions).

A

Methenamine (converted to formaldehyde only at an acidic pH; in the urine to treat UTI).

35
Q

Prodrug designed to increase the chemical stability of the active metabolite.

A

Hetacillin (converted to ampicillin)

36
Q

Prodrugs designed to improve the membrane permeability of its active metabolite.

A

Enalapril
Levodopa
Pivampicillin

37
Q

Progestin classified as a derivative of testosterone.

A

Ethisterone

38
Q

Progestin classified as a progesterone derivative.

A

Megesterol acetate

39
Q

Estrogen which is an estradiol metabolite originally obtained from the urine of pregnant mares.

A

Equillin sodium sulfate

40
Q

Drug which is a derivative of anilin and has analgesic and antipyretic properties. The FDA requires a warning label that reads as follows:
“Warning: Do not give to children under 3 years of age or use for more than 10 days unless directed by a physician.”

A

Acetaminophen

41
Q

Anti-inflammatory agent which is an arylanthanilic acid derivative that has a lower incidence of GI bleeding than aspirin and has been approved for use in the management of primary dysmennorrhea.

A

Mefenamic acid

42
Q

Anti-inflammatory analgesic which is an arylacetic derivative that is comparable to aspirin in the treatment of rhuematoid arthritis, which lower incidence of side effects. It has also been apporoved for use in primary dysmenorrhea.

A

Ibuprofen

43
Q

It is a non-classical folate antagonist that is structurally similar to methotrexate. It inhibits the enzyme dihydrofolate reductase and has been approved for the treatment of Pnuemocystis carinii in patients with AIDS.

A

Trimetexrate

44
Q

Dye which is a mixture of the chlorides of rosaniline and p-rosaniline. It is an ingredient of Castellani’s paint, which is used topically in the treatment of fungal infections, such as ringworm and athlete’s foot.

A

Basic fuchsin

45
Q

Dye which is available as vaginal suppositories for the treatment of yeast infections and has also been used orally as an antihelmintic for stroingyloides and oxyurias.

A

Methylrosaniline chloride

46
Q

Phenolic drug which has expectorant activity.

A

Guiacol

47
Q

Drug for diabetes that inhibit the enzyme a-amylase.

A

Acarbose

48
Q

Drug for diabetes that inhibit the enzyme a-glucosidase.

A

Miglitol

49
Q

Enzyme inhibited by Ethambutol.

A

Arabinosyl transferase

50
Q

Enzyme inhibited by Sildenafil.

A

3’,5’-cyclic GMP phoshodiesterase

51
Q

Enzyme inhibited by Physostigmine.

A

Acetylcholinesterase

52
Q

Condition which occurs when an agonist is bound to its receptor for a long peroid of time.

A

Desensitization

53
Q

Condition which occurs when antagonist is bound to its receptor for a long peroid of time.

A

Sensitization

54
Q

These are exogenous chemical messengers that act as antagonists, but also eliminate any resting activity associated with a receptor.

A

Inverse agonists

Organic Medicinal Chemistry (5 decks)

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