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Pharmacology drew > winter final > Flashcards

winter final Flashcards

1
Q

Chloroquine and Hydroxychloroquine

A

Blood Shizonticides anti malarial drug

  • acts on RBC form, no affect on tissue forms, affects the bugs ability to feed( cannot digest hemoglobin),drugs ability to raise ph of malarial food vacuoles, prophylaxis for all forms
  • clinical cure for all malaria, radical cure for falciparum and . malaria, resistant forms of falciparum are developing( transport pumps remove drug from the parasite
  • oral, well abs, accumulated in melanin rich tissues i.e. skin and retina, met in liver(caution in liver DS), 6-7d t.5
  • tox-less than quinine-dizzy headache tinitus, GI upset(take w/food), renal and corneal tox(monitor sight),
  • immunologic- skin rashes, blood dycrasias, lupus like syndrome, CONTRA IN pts with porphyria or psoriasis
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2
Q

Blood Shizonticides

A

Chloroquine
hydroxychloroquine
Quinine and Quinidine Gluconate
Mefloquine

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3
Q

special property of Hydroxychloroquine

A

Anti inflammatory at high doses

  • used in RA and Lupus
  • malaria dose is 310, Anti inflame dose is 400-600
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4
Q

Quinine and Quinidine Gluconate

A
  • anti malarial drug -Blood Shizonticides
  • MOA-interferes with plasmodial digestion of hemogllobin, used in chloroquine resistant Falciparum
  • found in cinchona bark -old drug, acts on all erythrocyte forms(schizonticidal forms), gametocytocidal in vivid and p. malaria,
  • oral, t.5=5-16 hours
  • other action- analgesia and antipyretic similar to aspirin, GI irritation-nvd, blurred vision, auditory deafness(tints and deafness)
  • tertogenic and abortion, depressant effect on heart, mild neuromuscular blockade

_cinchonism- syndrome of toxicity resembles salicylism- Headache, Nausea, dizzy, blurred vision, tinnitus)

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5
Q

Mefloquine

A
  • anti malarial drug -Blood Shizonticides
  • used in chloroquine resistant Falciparum treatment and prophylaxis, acts on all erythrocyte forms(schizonticidal forms)
  • MOA similar to chloroquine, interferes with plasmodial digestion of hemoglobin
  • rapid resistance in some strains, only oral b/c irritating, can use in preg
  • tox-seizures and aggravate latent psycosis- NO USE in pts w/ history of mental illness or epilepsy
  • potential cardiac (myocardial depression) and CNS toxicities, use caution in pts w/ cardiac psychiatric, or epilepsy disorders
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6
Q

inhibitors of folic acid synthesis and utilization

A

pyrimethamine

Proguanil

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7
Q

Artemisinin analogues

A

artemether plus lumafantrine - isolated from chinese herbal medicine

  • anti malarial drug -Blood Shizonticides
  • generates free radicles that kill paracyte
  • GI irritation and headache
  • Drug of choice in combo w/ pyrimethamine and sulfadoxone others to treat chloroquine resistant strains
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8
Q

pyrimethamine

A

anti malarial

inhibits DHFR mainly on the Erethrocyte forms, some affect on tissue and pre RBC stages and cryptomerozoites

  • prophylaxis for chloroquine resistant P.F strains
  • used in combo w/ sulfonamides PYRIMETHAMINE PLUS SULFADOXINE (-sulfonamide MOA- inhibit dihydropteroate synthase stoping conversion of PABA–> dihydropteroic acid) (used for presumptive treatment)
  • used w/ artemisinin analogues for CR P.F
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9
Q

Proguanil

A

anti malarial
casual prophylaxis treatment

inhibits DHFR mainly on the Erethrocyte forms, some affect on tissue and pre RBC stages and cryptomerozoites

  • prophylaxis for chloroquine resistant P.F strains
  • used in combo w/ sulfonamides PYRIMETHAMINE PLUS SULFADOXINE (-sulfonamide MOA- inhibit dihydropteroate synthase stoping conversion of PABA–> dihydropteroic acid) (used for presumptive treatment)
  • used w/ artemisinin analogues for CR P.F
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10
Q

Atovaquine plus proguanil

A

new combination anti malarial drug

  • atovaquone- acts to depolarize parasites MITO and inhibits E- transport
  • RARE SE- Headache and ab pain- not sure preg use
  • alternative to doxy and mefloquine prophylaxis against CR P.F, daily dose, rather expensive
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11
Q

tetracyclines

A

alternative anti malarial

broad spectrum bacteriostatic agent to inhibit protein synthesis by binding to the 30S subunit of ribosomes, and blocking amino acyl T-RNA to Bind and add AA

  • excreted via renal filter(10-50%), in bile
  • resistance- increased efflux pumps, Tet(AE) conver resistance to G- to tetra, doxy and minocycline, production of protein to prevent binding to 30S tet(M) ,enzymatic inactivation
  • USE-not 1st choice for G+, G- aerobes, or anaerobes
  • drugs of choice for- spirochetes(Lyme Ds), clamidia, Rickettsiae(RMSF)(DOXY), Mycoplasm pneumo, brucella, H pylori, peridontitis
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12
Q

tissue schizonticides

A

Primaquine

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13
Q

Primaquine

A

anti malarial -tissue schizonticides

  • active against tissue forms of all species of plasmodia, MAIN EFFECT IS TO KILL TISSUE FORMS OF VIVAX AND OVALE–> radical cure for these
  • gametocytocidal
  • little RBC form effect, not used for prophylaxis b/c of toxicities
  • TOX- mild w/ acute use, increased w/ chronic use
  • GI upset, CNS-headache and dizzyness, HEMOLYTIC ANEMIA- in G6PD pts, avoid in preg
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14
Q

preferred drugs to treat Enterobius vermicularis (pinworms

A

Albendazole

  • Pyrantel
  • rigid standards of personal hygiene
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15
Q

preferred drugs to treat Ascaris lumbricoides

A
  • 2nd most common in US, most common in world, night soil, wandering worms, surgery may be needed for wanders
  • asymptomatic infections-Albendazole
  • Heavy infections- Pyrantel(causes worm paralysis)
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16
Q

preferred drugs to treat hookworms (nectar americanus)

A

Albendazole,

-also used to treat creeping eruptions

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17
Q

preferred drugs to treat Tapeworms

A

drugs affect the scolex

  • T. Saginata(beef)= praziquantil
  • T solium (pork)= praziquantil( along with a purgative Mg sulfate)
  • Neurocysticercosis-dexamethazone2 d b4 anti helminth and albendazole and prazaquantil
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18
Q

Albendazole

A

anti helminth drug

5% orally absorbed and metabolite from liver responsible for systemic effects

  • MOA- binds to free B tubulin, inhibits microtubule polymerization and microtubule dependent Glucose uptake, doesn’t bind well to human B tubulin
  • NVD, teratogenic potential, can resign LFTs and Leukopenia
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19
Q

Pyrantel

A

available OTC, anti helminth, Broad spec used against many nemotodes

  • MOA-activation of the cholinergic nicotinic receptor in the muscle of nematodes-> depolarizing muscular blockade-> worms become paralyzed and expelled from GI tract
  • GI most common-NV cramps, RARE but serious liver failure, use in preg and child
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20
Q

Praziquantel

A
  • oral with wide tissue breakdown including CNS, metabolite and drug eliminated in kidney
  • works again Neuroshistosomiasis, broad spec against schistosomes(trematodes) and tapeworms

–MOA-induces muscle contraction and spastic paralysis of the musculature of worms via increased calcium ion influx, with cestadoes causes the sucker to become dislodged

SE- Dizzy drowsy Headache, decreased alertness are most common, GI NV ab pain, increased LFTs, avoid with preg, low grade fever and rash

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21
Q

Antiprotozoals

A 
Metronidazole
Idoquinol
Paromomycin
Nitazoxanide
-opportunistic infections with protozoa are prominent in infants, individuals with cancer, transplant recipients, those receiving immunosuppressive drugs, and persons with acquired immunodeficiency syndrome (AIDS)
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22
Q

preferred drugs entamoeba histolytica

A

Idoquinol, paromomycin-asymptomatic carriers(luminal drugs)-

-symptomatic(tissue amebiside and Luminal acting drugs)) metronidazole plus Idoquinol or paromomycin

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23
Q

preferred drugs for Giardia

A
  • metronidazole

- nitazoxanide

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24
Q

preferred drugs for cryptosporidiosis

A

nitazoxamide

-paromomycin

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25
Q

metronidazole

A
  • good oral and so not used in luminal phase, used in symptomatic pts
  • MOA- Cidal drug, gets reduced w/in and binds to intracellular macromolecules( DNA)–> inhibits DNA synthesis

-uses- anaerobic bacteria Bacteroides fragilis and the gram positive rod Clostridium difficile.
protozoans entomeba histolytica, Trichomonas vaginalis, and Giardia lamblia

-SE-disulfram like interaction with alcohol, increases effect of oral anticoags, Nausea , headache, dry mouth, vomit Dhrea, carcinogenic in rodents

26
Q

Iodoquinol

A

luminal or contact amebicide

-MOA- unknown, not well absorbed and excreted in feces

USE- sed in combination with
Metronidazole to treat symptomatic infections and used alone to treat asymptomatic carriers.

-SE-neurotoxinc if given >2g/day for > 20 days, loss of vision and optic neuritis, safe inpreg

27
Q

Paromomycin sulfate

A

anti amoeba

  • poor oral abs most excreted in feces,luminal or contact amebicide
  • MOA- aminoglycoside–> inihbits protein synthesis via binding to the 30 S subunit
  • Uses- E histolytic-(alone for asymptomatic, in combo w/ metronadazole for symptomatic or extraluminal amebiasis
  • Drug of choice in AIDS pts w/ cryptosporodiosis
  • se-GI-anorexia NV increased motility, abdominal cramping, nephron and ototox and neuromuscular blockade
28
Q

Nitazoxanide

A

MOA- converted first to active metabolite tizoxanide

  • interferes with anaerobic energy metabolism by inhibiting pyruvate:ferredoxin 2-oxidoreductase enzyme dependent electron transfer reaction which is important for organisms dependent on anaerobic metabolism (e.g. Cryptosporidium parvum, Giardia lamblia)
  • USE- dhrea from crypto in immunocompetent children1-11 yo, adolescent and adults

USE- dhrea from giardia in pts >1yo

SE-ab pain , dhrea, N and headache
no mutogentic/carcinogenic effects( unlike metronidazole)

29
Q

alkylating agents

A 
-CCNS, cells most susceptible in late G1 and S
Mechlorethamine 
Cyclophosphamide 
Carmustine 
Cisplatin

able to transfer reactive alkyl group to DNA-> cytotoxic effect, alkylation of DNA reacts w/ N7 on Guanine and alkylated purine,

  • miscoding of DNA, incomplete repair, leads to cross linking of DNA strands and inability for separate
  • toxicity-vessicant at injection, acute-NV phlebitis, chronic- bone marrow supression
30
Q

Mechlorethamine hydrochloride

A

anti cancer drug, alkalating agent

  • forms cross links between DNA, at the N7 of guanine,
  • results in miscoding of DNA, incomplete repair of alkylated segments, excessive cross linking and inability to separate

nitrogen mustard, bis chlorethyl amine
CCNS- M and G1 most sensitive

–toxicity-vessicant at injection, acute-NV phlebitis, chronic- bone marrow supression

31
Q

Cyclophosphamide (CTX)

A

CCNS,anti cancer drug
derivative of Mechlorethamine, requires activation by P450 to active metabolite ALDOPHOSPHAMIDE

  • forms cross links between DNA, at the N7 of guanine,
  • results in miscoding of DNA, incomplete repair of alkylated segments, excessive cross linking and inability to separate

-USE acute chronic leukemia, immunosupressive-RA, transplant

–toxicity-vessicant at injection, acute-NV phlebitis, chronic- bone marrow supression

32
Q

Carmustine

A

Nitrosurea, CCNS anti cancer drug (BCNU)

_bifunctional alkylator , nonspecific, highly lip soluble

_USE- Brain tumors, hodgkins and non hodgkins lymphomas

–toxicity, acute-NV phlebitis, chronic- leukopenia and thrombocytopenia

33
Q

Cisplatin

A

CCNS anti cancer drug

  • Platinum complex, G1 most specific(STILL CCNS),
  • bifunctional alkylating agent, inter and intra strand cross linking, disrupts double helix

-TOX-Nephrotoxic and ototoxic
also acute-NV phlebitis, chronic- bone marrow supression

34
Q

Antimetabolites

A 
-CCS agents
Methotrexate
Mercaptopurine
Fluorouracil
Cytarabine

-metabolized instead of normal substrate, compete with normal metabolites, affect nucleotide and nucleic acid synthesis

35
Q

Methotrexate

A
  • CCS agent S phase -anti cancer drug, folic acid analogue
  • MOA- inhibits DHFR-> blocking folic acid synthesis–> inability to convert deoxyuridylate to thymidylate
  • leucovorin(foilinic acid) protects normal cells
  • poor CNS penetrate, 50% BOUND TO PLASMA PROTEIN
  • TOX- acute-NVD, delayed- BM suppression, go/oral ulcer, alopecia, hepatotox
  • USE- leukemia and psoriasis and RA
36
Q

Mercaptopurine

A

CCS agent S phase, Purine analogue, sulfhydryl substituted analogue of hypoxanthine

-MOA- inhibts enzymes of purine interconversion–> purine nucleoside systhesis inhibition, converted by HGPRT to 6-thioinosinic acid

—metabolized by xanthine oxidase—-

-toX- cute-NVD, delayed- BM suppression, cholestatic jaundice

37
Q

Fluorouracil

A

pyrimidine analogue
CSS anti cancer agent, S phase,

  • converted to 5-deoxyuridine-> binds to thymidylate synthetase covalently, blocks conversion of deoxyuridylate to thymidylate the rate limiting step in DNA synthesis
  • no acue tox, -nausea oral ulcers and BM supression
38
Q

Cytarabine

A

pyrimidine analogue
CSS S pahse anti cancer agent,

  • converted to cytarabine triphosphate inhibiting DNA polymerase via compete w/ deoxycitidine triphosphate
  • Delayed TOX- NV BM suppress, megaloblastosis, leukopenia, thrombocytopenia
39
Q

Natural anti cancer products

A

Anthracycline Antibiotics: Daunorubicin Hydrochloride, Doxorubicin Hydrochloride

Vinca Alkaloids, Epipodophylotoxins and Taxanes: Vinblastine Sulfate, Vincristine Sulfate, Etoposide, Paclitaxel

40
Q

Anthracycline

A

antibiotic anticancer drugs CCNS( but most effective in S phase)
Daunorubicin Hydrochloride, Doxorubicin Hydrochloride

  • MOA- intercalate and bind to DNA–> unwinding of DNA–> destroy the DNA template, anti tumor activity at tetracycline ring
  • TOX- Acute- NV, red urine, tissue necrosis, delayed- BM suppression, CARDIOMYOPATHY
  • USE- used in combination with other drugs to synergize effects
41
Q

Vinblastine sulfate

A

CCS M phase specific anti cancer drug

  • MOA- bind to tubulin and disrupt the mitotic spindle, prevents segregation of chromosomes in metaphase
  • TOX-acute- NV PHLEBITIS, DELAYED-neurologic( peripheral neuropahty and BM depression
42
Q

Vincristine sulfate

A

CCS M phase specific anti cancer drug

  • MOA- bind to tubulin and disrupt the mitotic spindle, prevents segregation of chromosomes in metaphase
  • TOX-acute-local reactivity, DELAYED-neurologic (peripheral neuropahty), constipation andalopecia and mild BM depression
43
Q

Etoposide

A

CCS for G2 phase anti cancer drug

derivative of podophyllotoxin- MOA forms complexes with topoisomerase II and DNA–>DNA breaks w/o resealing–> cell death

-TOX- A- NVD D- leukopenia, alopecia

44
Q

Paclitaxel

A

CCS anti cancer drug specific to M and G2 phase from bark of yew tree

  • MOA- antimicrotubule agent, rather than inhibit microtubule assembly like vincristine and vinblastine it promotes microtubule assembly to stabilize membranes
  • TOX- A: NV D- BM suppression, hypersensativity , peripheral neuropathy, alopecia
45
Q

Prednisone

dexamethazone

A

adrenocorticosteroid

MOA- Binds to cytosolic receptors (complex) and affect DNA and RNA and protein synthesis
2. Suppresses lymphocytes and macrophages

TOX- CUSHINGS SYNDROME

46
Q

Tamoifen

A

CCS agent specific to G1 phase, non steroids anti estrogen

MOA- competitive inhibitor of estrogen inhibitor in estrogen sensative tissues-> receptors are nuclear transcription factors

  • tox- most common are menopausal
  • short term- hot flash fatigue, NV, vag dryness
  • LONG term- visual disturbance, vag bleed, ocular tox, thrombotic effect, thrombocyto/leukopenia
  • MOST SERIOUS- possible tumor promoting, endometrial cancer

-USE- Estrogen R positive breast cancer, reduces risk of recurrence of breast cancers

47
Q

imatinib mesylate

A

tyrosine kinase inhibitor CCS at G1 phase

  • inibits Bcr-Abl tyrosine kinase inhibitor preventing phosphorylation, inhibits cell proliferation and induce apoptosis in leukemia and CML
  • TOX- A- ab pain NVD, D- fatigue joint pain, muscle pain

USE-acute lymphocytic leukemia, Ph+ chronic myeloid Leukemia

48
Q

Trastuzumab

A

monoclonal AB, CCS at G1 phase

  • Humanized monoclonal Ab that binds to human epidermal growth factor(EGF) Her-2, blocking EGF and down regulating receptors tyrosine kinase activity, causing G1 cycle arrest
  • TOX- A-NVD, D- anemia, neutropenia, infection, fatigue

_USE- adjuvant in breast cancer w/ overexertion of HER-2, metastatic breast cancer-in combo w/ paclitaxel first line for HER-2 overexpressing cancer

49
Q

amphetamine

A

CNS effects- stimulation and increased arousal and stir via reticular activating system
-euphoria - some may get paranoid and dysphoria
-delay in fatigue induce decline in performance
-rebound effect
-psychological and physical dependence, withdraw symptoms of fatigue lethargy and depression
-amphetamine psycosis- similar to schizo
-supressed apatite
this card sucks

50
Q

d-amphetamine

A

sympathomimetic effects and toxicities
this and amphetamine- irreversible degeneration of dopamine and serotonin pathways

MOA- enhanced release and (lesser effect ) to decrease re uptake of NE and DA, stimulate direct reward centers, decreased levels of DA in reward centers(chronic)

-MET- enhanced excretion in acidic urine

51
Q

Lisdexafetamine

A

prodrug amphetamine bound to lysine

moderate rate of conversion leading to a lower abuse potential

-USed in ADHD

52
Q

methamphetamine

A

presence of methyl group increases lipid absorption and increases lipid solubility, produce intense effect on brain and widely abused

53
Q

methylphenidate

A

similar to amphetamine used in the treatment of ADD, has a paradoxical effect and effects the locus creels and increase focus attention

54
Q

Cathinone

A

found in the leaves of the Khat plant of east africa and the middle east

-most recently synthetic form has marketed as bath salts

55
Q

ephedrine

A

natural product found in herbal preps, has sympathomemetic actions

56
Q

Modafanil

A

newer drug for narcolepsy and shift work disorder

MOA unclear, technically not amphetamines but have similar effects

57
Q

armodafanil

A

newer drug for narcolepsy and shift work disorder

MOA unclear, technically not amphetamines but have similar effects

58
Q

Cocaine

A

a hell of a drug

59
Q

caffiene

A

methylxanthine with some effects

this and theophylline used to treat apnea in preterm infants

60
Q

strychnine

A

spinal cord stimulant
potent convulsant in rat poison
-antagonist at glycine receptors the spinal cord and other CNS areas, removing post synaptic inhibitory property–> toxic seizures

treatment - symptomatic and diazepam to control seizure

61
Q

tetanus toxin

A

spinal cord stimulate fro clostridium

  • produces generalized tetanus and tonic convulsions similar to strychnine
  • inhibits the release of glycine from renshaw cells in SC

-treatment-symptomatic and diazepam for seizures and appropriate anti microbe therapy

62
Q

Preferred drug for Trichomonas vaginalis

A

metronidazole

Pharmacology drew (9 decks)

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