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Pmcol 344 drugs Flashcards

1
Q

Omeprazole

A

tx of ulcers - proton pump inhibitor
irreversible = long acting (T1/2 = 1 hr but effects last 2-3 days)
weak base → ionized form accumulates outside cell in acid = promotes conversion of prodrug
inhibits some CYP450 enz = potentiation of drug actions ex. warfarin phenytoin, benzos, TCAs

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2
Q

Cimetidine

A

tx of ulcers- H2 receptor antagonist (Kd H2 = 0.80 uM)
given orally, ↓ basal + stimulated acid secretion by >90% = ↑ pH above 4 (↓ pepsin activity)
promotes healing of ulcers
inhibits some CYP450 enz = potentiation of drug actions ex. warfarin phenytoin, benzos, TCAs
can cause reversible gynaecomastia in men (affinity for E Rs = ↑ prolactin secretion)

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3
Q

alginates

A

tx of ulcers- antacid
neg charged polysaccharides from algal cell walls
absorb water to form viscous gum (possibly ↑ viscosity + adherence of mucus to stomach lining)

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4
Q

bismuth chelate

A

tx of ulcers - protect mucosa
colloid
used with triple therapy to tx H.pylori → kills bacteria + prevents adherence

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5
Q

sucralfate

A

tx of ulcers - protect mucosa
complex of Al(OH)3 + sulfated sucrose
release Al in acidic envir to leave neg-charged complex = binds to proteins + glycoproteins in mucus to form gel

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6
Q

Misoprostol

A

tx of ulcers - protect mucosa
stable PGE1 analog (reduced metabolism by oxidation)
- mucosal cells: EP1/2 Rs = ↑ HCO3- ; EP4 Rs = ↑ mucus prod.
- ECL cells: EP2/3 Rs (inhibit AC) = inhibit histamine prod.
- inhibits HCl release from parietal cells
- enhances mucosal blood flow
antagonizes effects of NSAIDs = prevents damage/promotes healing
contraindicated in pregnancy (stimulates contractions)

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7
Q

Ipecac

A

emetic drug

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8
Q

Hyoscine

A

anti-emetic - mAChR antagonist
acts at vomiting centre + vestibular nuclei
given prophylactically for motion sickness + post-op emesis)
predictable side effects: dry mouth, blurred vision, sedation, constipation

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9
Q

Cisplatin (GIT)

A

chemo agent
releases 5HT from enterochromaffin cells in GIT + stimulates CTZ/visceral nerves
= chemo-induced emesis

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10
Q

Ondansetron

A

anti-emetic - 5HT3 R antagonist
acts at CTZ + visceral afferents
used for chemo-induced emesis; less effective against motion sickness
CV side effects → Long QT syndrome

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11
Q

Metoclopramide

A

anti-emetic - D2R antagonist
CTZ is primary site of action
used for chemo-induced vomiting but less effective than 5HT-3 antagonists
can cross BBB = mvt disorders

tx of constipation
↑ gastric emptying → relaxes pyloric sphincter + smooth muscle
↓ absorption of drugs normally absorbed in stomach (weak acids)

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12
Q

Domperidone

A

anti-emetic - D2R antagonist
does not cross BBB = no CNS effects
does ↑ gut motility

tx of constipation

stimulate lactation in new mothers
inhibits hypothalamic tonic DA release → pituitary lactotrophs = stimulate prolactin release

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13
Q

Chlopromazine

A

antipsychotic phenothiazine
anti-emetic
tx of severe nausea + vomiting associated with cancer, radiation therapy, cytotoxic drugs opioids, anesthetics
D2R antagonist → acts in CTZ + blocks histamine + muscarinic receptors
limited by unwanted effects = used as last resort

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14
Q

Nabilone

A

cannabinoid
anti-emetic
acts in CTZ to suppress output

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15
Q

Dexamethasone

A

glucocorticoid
anti-emetic
used with chemo; unclear mechanism

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16
Q

Aprepitant

A

NK1 R antagonist
anti-emetic
action at CTZ + vomiting centre
used in combination with dexamethasone + ondansetron for chemo-induced emesis

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17
Q

Atropine

A

tx of diarrhea - muscarinic antagonist
block action of ACh = relax gut muscle + ↓ motility

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18
Q

Morphine

A

tx of diarrhea - opiate
major unwanted effect is constipation
also Codeine, Diphenoxalate
CNS effects

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19
Q

Loperamide

A

tx of diarrhea - opiate
structurally similar to Pethidine (synthetic opioid agonist) but does not cross BBB
only peripheral effects
commonly used for travellers diarrhea (↓ frequency of cramps, ↓ duration of illness but can cause constipation)

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20
Q

Lactulose

A

tx of constipation - osmotic laxative
disaccharide of fructose + galactose, macrogols

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21
Q

Bisacodyl

A

tx of constipation - stimulant laxative
given as a suppository
can stimulate defecation in 15 minutes

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22
Q

Senna

A

tx of constipation - stimulant laxative
active component (glycoside) directly stimulates cholinergic nerves in myenteric plexus = ↑ peristalsis + defecation
used in combination with stool softeners for chronic opioin-induced constipation

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23
Q

Docusate

A

stool-softener

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24
Q

Cisapride

A

tx of constipation - 5HT4 agonist
enhancement of ACh release
blocks cardiac HERG channels = fatal cardiac arrhythmias (LQT syndrome)
also Tegaserod

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25
Prucalopride
tx of constipation - 5HT4 agonist not linked to ↑ risk of cardiac events
26
Lubiprostone
tx of constipation-dominant IBS PGE1 analogue → EP4 receptor = ↑ cAMP to activate CFTR → Cl- efflux = stimulates fluid secretion ↑ fluid in stool → stretches gut + speeds up transit of gut contents poorly absorbed = selective for gut
27
Prednisolone
tx for UC/Crohn's glucocorticoid binds members of nuclear receptor superfamily = modify gene transcription = inhibit stages of inflammatory process mild = rectal enemas (restricted action) severe = oral long term = ↓ immune system
28
Sulfasalazine
tx for UC/Crohn's aminosalicylate = maintenance of remission for both disorders not well absorbed in gut; bacteria in colon release active (5-aminosalicylic acid; mesalazine) localized anti-inflammatory agent; scavenge free radicals; inhibit PG synthesis
29
Infliximab
IBD biologic tx target components of inflammatory pathway: Anti-tumor necrosis factor-α (TNF-α)
30
Adalimumab
IBD biologic tx target components of inflammatory pathway: Anti-tumor necrosis factor-α (TNF-α)
31
Golimumab
IBD biologic tx target components of inflammatory pathway: Anti-tumor necrosis factor-α (TNF-α)
32
Vedolizumab
IBD biologic tx target components of inflammatory pathway: Anti-α4β7 integrin on T-helper lymphocytes
33
Ustekinumab
IBD biologic tx target components of inflammatory pathway: Anti-protein subunit of interleukin-12 + IL-23 → blocks interleukin binding to IL-12Rβ1 receptors on immune cells
34
Acetylsalicylic acid
anti-platelet drug non-selective NSAID with anti-platelet effects orally active, low dose enough to inhibit platelet fxn irreversibly acetylates + inhibits COX-1 = prevent TXA2 (potent platelet aggregation stimulator) synthesis inhibition lasts for life span of platelets unwanted effects: GI bleeding, ↓ hemostatic fxn, hypersensitivity in asthma/nasal polyps, Reye's syndrome, ↓ glomerular filtration rate, mild hepatitis
35
Ticlopidine
anti-platelet drug first thienopyridine can cause neutropenia + thrombocytopenia (↓ neutrophils; platelets) largely replaced by clopidogrel
36
Clopidogrel
anti-platelet drug thienopyridine more selective for P2Y12 = less side effects often used by ASA intolerant individuals oral admin → quick metabolism (~5hrs) by CYP2C19 - pts with variant allele = no conversion to active form side effects: dyspepsia, rash, diarrhea
37
Prasugrel
anti-platelet drug newest thienopyridine faster biotransformation (~30 min) to active metabolite more efficacious as anti-platelet drug but more bleeding
38
Ticagrelor
anti-platelet drug cyclo-pentul-triazolo-pyrimidine orally active (not prodrug), reversible allosteric P2Y12 antagonist adverse effects: dyspnea, bradyarrhythmia
39
Dipyridamole
anti-platelet drug cyclic nucleotide phosphodiesterase inhibitor = prevents breakdown of cAMP/cGMP → continuous inhibition of platelet aggregation also blocks adenosine uptake; ↓ platelet TXA2 / ↑ endothelial PGI2 synthesis not effective alone → used with ASA to prevent TIA + stroke
40
Abciximab
anti-platelet drug glycoprotein IIb/IIIa antagonist mouse/human chimeric monoclonal antibody against receptor protein
41
Eptifibatide
anti-platelet drug glycoprotein IIb/IIIa antagonist synthetic cyclic heptapeptide based on Arg-Gly-Asp sequence
42
Tirofiban
anti-platelet drug glycoprotein IIb/IIIa antagonist synthetic non-peptide based on Arg-Gly-Asp sequence
43
Warfarin
anti-coagulant derived from sweet clover, developed as rat poison oral vitamin K reductase antagonist = stops coagulation cascade interferes with carboxylation of glutamic acid residues in clotting factors II, VII, IX, X leads to accumulation of inactive clotting factors that cannot bind to neg surfaces via Ca2+ lots of problems
44
unfractionated Heparin
anti-coagulant favours thrombin inhibition
45
low molecular weight Heparin
anti-coagulant favours Xa inhibition more favourable pharmacokinetics - longer elimination half-life = less frequent dosing + more predictable anticoagulation effects
46
Ribaroxaban
anti-coagulant reversible, direct competitive inhibitor of factor Xa (high selectivity) orally active drug, once daily dosing unwanted effects: bleeding; contraindicated in pts with renal failure + Apixiban + Edoxaban
47
Dabigatran Etexilate
anti-coagulant reversible direct competitive inhibitor of thrombin orally active prodrug; once/twice daily dosing rapidly converted by plasma esterases to dabigatran unwanted effects: bleeding; contraindicated in pts with renal failure
48
Hirudin
anti-coagulant from medicinal leech specific inhibitor of thrombin 7 KDa protein (65 amino acids) does not need ATIII slowly reversible
49
Lepirudin
anti-coagulant recombinant hirudin (thrombin inhibition)
50
Bivalirudin
anti-coagulant shortened (20aa) hirudin-based synthetic peptide (thrombin inhibition)
51
Alteplase, Duteplase, Reteplase
thrombolytic/fibrinolytic drug recombinant tissue-plasminogen activator IV admin converts plasminogen to plasmin → breaks down fibrin = clot lysis tx of stroke
52
Streptokinase
thrombolytic/ fibrinolytic drug non-enzymatic protein from hemolytic streptococci allows plasminogen to gain enzymatic activity by forming stable complex to induce conformational change + expose active site) → breakdown fibrin inactivated by anti-streptokinase antibodies
53
Mechlorethamine
Nitrogen mustard (alkylating agent) myelosuppression Hodgkin's lymphoma
54
Chlorambucil
Nitrogen mustard (alkylating agent) myelosuppression Chronic lymphocytic leukemia
55
Melphalan
Nitrogen mustard (alkylating agent) myelosuppression multiple myeloma
56
Cyclophosphamide
Nitrogen mustard (alkylating agent) prodrug (metabolized by hepatic cytochrome oxidase) active = acrolein + phosphoramide mustard myelosuppression + immunosuppression + hemorrhagic cystitis lymphoid + myeloid malignancies
57
Acrolein
metabolite of cyclophosphamide cytotoxic = lung irritant + hemorrhagic cystitis doesn't target cancer cells, causes side effects
58
Ifosfamide
Nitrogen mustard (alkylating agent) myelosuppression hemorrhagic cystitis → always given with MESNA lymphoid + myeloid malignancies
59
Mesna
mercaptoethanesulfonate given with cyclophosphamide/ ifosfamide to prevent hemorrhagic cystitis inactivates acrolein → detoxification
60
Carmustine
Nitrosourea (bifunctional alkylating agent) activated in liver myelosuppression + leukemogenic + hepatoxicity
61
Lomustine
Nitrosourea (monofunctional alkylating agent) activated in liver myelosuppression + leukemogenic + hepatoxicity
62
Busulfan
Alkyl sulfonate (bifunctional alkylating agent) = intra-strand crosslinks myelosuppression used in high doses for bone marrow transplants
63
Dacarbazine
Triazine (alkylating agent) active myelosuppression glioblastomas + melanomas
64
Temozolomide
Triazine (alkylating agent) prodrug → metabolized to Dacarbazine myelosuppression glioblastomas + melanomas
65
Thiotepa
Ethylenimine (alkylating agent) myelosuppression lymphomas; breast, ovary, bladder cancer; malignant effusions
66
Cisplatin
bifunctional alkylating agent forms intrastrand crosslinks nephrotoxicity (generation of ROS) testicular, ovarian, solid tumour cancers cell-cycle non-specific
67
Methotrexate
anti-folate (antimetabolite) blocks DHFR of folate cycle polyglutamated = also blocks TYMS (↑ efficacy) cytotoxicity = S phase myelosuppression + GI ulcers + pulmonary effects breast cancer, childhood acute lymphoblastic leukemia, osteogenic sarcoma
68
Leucovorin
rescues normal tissue from MTX toxicity DHFR-independent conversion to FH4 only taken up in normal cells = used for tx of osteosarcoma
69
Fluorouracil
pyrimidine analogue (antimetabolite) nucleobase analogue → becomes FdUMP = inhibits TS (similar anti-folate effect as MTX) cytotoxicity = S phase myelosuppression + GI toxicity breast cancer + colorectal cancers IV admin
70
Capecitabine
prodrug of 5-FU selectivity: enzyme for metabolism is upreg in tumor cells = higher levels of 5-FU produced oral admin = replace for tx of gastric cancers
71
Raltitrexed
specific thymidylate synthase inhibitor inhibits DNA synthesis → deplete dTMP cytotoxicity = S phase tx of colorectal cancer
72
Cytarabine
pyrimidine analogue (antimetabolite) nucleoside analogue prodrug rapid deamination + clearance competitive inhibitor of DNA polymerase cytotoxicity = S phase myelosuppression acute myeloid leukemia (combined with an anthracycline drug) long IV infusions
73
Gemcitabine
pyrimidine analogue (antimetabolite) nucleoside analogue prodrug inhibits DNA polymerization, inhibits ribonucleotide reductase cytotoxicity = S phase myelosuppression solid tumors - pancreas, lung, breast
74
Fludarabine
purine analogue (antimetabolite) nucleotide analogue inhibition of DNA polymerase + ligase, ribonucleotide reductase, RNA polymerase = prevents elongation of DNA cytotoxicity = S phase (but also resting cells) immunosuppression CLL
75
6-Mercaptopurine
purine analogue (antimetabolite) nucleobase analogue → converted into fraudulent nucleotides inhibits enzymes cytotoxicity = S phase myelosuppression acute lymphoblastic leukemia
76
6-Thioguanine
purine analogue (antimetabolite) nucleobase analogue → converted into fraudulent nucleotides inhibits enzymes cytotoxicity = S phase myelosuppression acute lymphoblastic leukemia
77
Camptothecin
topoisomerase Ib inhibitor binds to topI-DNA complex = prevent DNA religation by top causes DNA ss breaks → apoptosis problems: low solubility + adverse drug reactions
78
Irinotecan
topoisomerase Ib inhibitor semisynthetic analog of camptothecin (substitution of A ring to ↑ solubility) prodrug: activated by carboxyesterase to SN-38 colon cancer
79
Topotecan
topoisomerase Ib inhibitor semisynthetic analog of camptothecin (substitution of A ring to ↑ solubility) prodrug ovarian + lung cancer
80
Doxorubicin
topoisomerase II inhibitor (anthracyclin)
81
Daunorubicin
topoisomerase II inhibitor (anthracyclin) solid tumors, leukemia, lymphoma
82
Idarubicin
topoisomerase II inhibitor (anthracyclin) AML
83
Epirubicin
topoisomerase II inhibitor (anthracyclin) breast cancer
84
Valrubicin
topoisomerase II inhibitor (anthracyclin) bladder cancer
85
Dexrazoxane
type II topoisomerase inhibitor (anthracyclin) inhibit ATP hydrolysis and DNA release at last step reduce adverse CV effects for doxorubicin breast cancer tx → iron chelating (antioxidant) activity
86
Carvedilol
adrenoceptor blocker antioxidant in cardiac tissue co-admin with doxorubicin to ↓ cardiotoxicity
87
Anthraquinones
act like anthracyclines but with fewer adverse effects/toxicities
88
Etoposide
podophyllotoxin derivatives (topoisomerase inhibitor) late S/early G2 *myelosuppression testicular, lung cancer; acute myeloid leukemia
89
Teniposide
podophyllotoxin derivatives (topoisomerase inhibitor) late S/early G2 *myelosuppression testicular, lung cancer; acute myeloid leukemia better cell accumulation
90
Vinblastine
antimicrotubular agent (vinca alkaloid) myelosuppression Hodgkin's lymphoma, non-small cell lung cancer
91
Vincristine
antimicrotubular agent (vinca alkaloid) peripheral neuropathy ALL, Hodgkin's lymphoma, pediatric solid tumors
92
Paclitaxel
antimicrotubular agent (taxane) ovarian, breast cancer; lung cancer
93
Docetaxel
antimicrotubular agent (taxane) higher affinity for tubulin binding site than Paclitaxel (↓ dose needed) myelosuppression ovarian, breast cancer
94
Noscapine
antimicrotubular agent sigma opioid receptor agonist used orally ↓ side effects + ↓ efflux (less resistance)
95
Tamoxifen
competitive inhibitor of estradiol binding to the ER in breast tissue prodrug, metabolized in liver by CYP2D6 (higher indiv variability) tx of ER+ and PR+ breast cancer prophylaxis for high risk of breast cancer development side effects: hot flashes (treated with SSRIs), ↑ risk of endometrial cancer, thrombosis
96
Raloxifene
non steroidal selective estrogen receptor modifier anti-E action on uterus and breast = tx for ER+ breast cancer w/o ↑ risk of endometrial cancer agonist action on bone → tx / prevention of osteoporosis in post-menopausal women
97
Anastrazole
selective aromatase inhibitor = ↓ E2 in body 2nd line hormonal therapy for breast cancer
98
Leuprolide
GnRH agonist R desensitization = block the secretion of LH from pituitary = inhibition of testosterone synthesis in testis
99
Degarelix
GnRH antagonist
100
Abiraterone
androgen synthesis inhibitor inhibits CYP17A1 (expressed in testicular, adrenal, and prostatic tumor tissues) blocks conversion of pregnenolone into 17ahydroxy derivative + subsequent formation of DHEA and antrostenedione used in castration-resistant prostate cancer
101
Flutamide
non-steroidal antiandrogen prodrug → metabolized to 2-OH flutamide = blocks binding of androgens at AR adverse effects: diarrhea, nausea, vomiting; liver function abnormalities usually administered with leuprolide
102
Enzalutamide
androgen receptor antagonist prevents binding of AR to DNA + AR coactivator proteins tx of castration-resistant prostate cancer
103
Herceptin
binds extracellular domain of HER2 R → blocks receptor dimerization + downstream signaling arrest cells in G1 phase suppresses angiogenesis used in combo with chemo
104
Cetuximab
MCAB against extracellular domain stimulates EGFR internalization
105
Panitumumab
MCAB against extracellular domain fully monoclonal antibody to EGFR
106
Imatinib
targets BCR-ABL tyrosine kinase tx of chronic myeloid leukemia competitively binds to site = inhibits protein → substrate cannot enter kinase site = tumor cell cannot proliferate
107
Nilotinib
second gen tyrosine kinase inhibitor active against imatinib-resistant patients
108
Gefitinib (Iressa)
ATP site competitive inhibitor of EGFR TK activity effectively inhibits HER1-HER2 heterodimers non-small cell lung cancer → low efficacy = no longer used as first line tx
109
Erlotinib (Tarceva)
EGFR inhibitor more effective for non-small cell lung cancer
110
Lapatinib
dual EGFR/ErbB inhibitor
111
Avastin (Bevacizumab)
angiogenesis inhibitor tx of metastatic colorectal cancer administered with chemo ex. 5-FU
112
Bortezomib
proteasome inhibitor B atom binds catalytic site of proteasome with high affinity + selectivity prevents degradation of pro-apototic factors = cell cycle arrest + apoptosis tx of relapsed multiple myeloma *myelosuppression + peripheral neuropathies
113
Marizomib
irreversible proteasome inhibitor less myelosuppression and peripheral neuropathy

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