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YEAR 2 - Principles of Pathology > Drugs list > Flashcards

Drugs list Flashcards

1
Q

What is the action and some features of aciclovir?

A
  • Guanosine analogue. Converted by viral thymidine kinase (but not human thymidine kinase) to aciclovir triphosphate, which inhibits DNA polymerase in infected cells.
  • During DNA synthesis mediated by the infection, the acyclovir triphosphate is incorporated into the chain
  • This terminates synthesis because there is no 3’ carbon on the acyclovir, so no more nucleotides can be added to the chain
  • This prevents the virus from completing the cycle
  • This is selectively toxic to the virus because the human cell can differentiate between the guanosine and the acyclovir
  • Used against HSV-1 and HHV-3 (varicella zoster) herpesviruses.
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2
Q

What is the action and some features of adrenaline in reference to immunopathology?

A
  • Strong β-adrenoreceptor agonist
  • Immediate treatment for type 1 hypersensitivity reactions
  • Asthma, acutely - acts at β2, bronchodilatory.
  • Anaphylaxis - strong vasoconstrictor, counters the systemic vasodilation to prevent vasodilatory shock
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3
Q

What is the action and some features of amoxicillin?

A
  • Type of penicillin
  • β-lactam antibiotic.
  • Binds to and inhibits penicillin-binding proteins (PBP) - transpeptidases involved in peptidoglycan synthesis.
    • They are structural analogues of the peptide cross-bridges in peptidoglycan
    • Therefore, they can preferentially bind to the transpeptidase enzymes (one of the penicillin binding proteins PBPs)
    • This stops transpeptidation, so the peptidoglycan cannot form
  • BACTERICIDAL
  • More effective against Gram +ve bacteria as target more accessible
  • Resistance seen in some bacteria through beta-lactamases
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4
Q

What is the action and some features of aspirin?

A
  • Cyclooxygenase I and II non-competitive, irreversible inhibitor, acetylates them.
  • Reduces synthesis of prostaglandins, reduces inflammation. Prostaglandins sensitise C-fibre pain neurons so aspirin reduces inflammatory pain. NSAID.
  • As a NSAID, used in chronic inflammatory diseases such as rheumatoid arthritis.
  • Causes ototoxicity at high doses.
  • Low doses: mild indigestion, risk of bleeding
  • Reduces synthesis of thromboxane A2, a major platelet activator and stimulator of aggregation. Of the antiplatelet agent class of anticoagulants as platelets have no nucleus so cannot synthesise more COX once inhibited.
  • Given long-term for prophylactic prevention of clotting for those at risk, or acutely after MI to reduce risk of clots.
  • Problems of long-term aspirin:
    • Liver/kidney disease
    • Uncontrolled bleeding
    • GI problems
    • Aspirin allergies
    • Doesn’t mix well with alcohol
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5
Q

What is the action and some features of benzylpenicillin?

A
  • Type of penicillin
  • β-lactam antibiotic.
  • Binds to and inhibits penicillin-binding proteins (PBP) - transpeptidases involved in peptidoglycan synthesis.
  • They are structural analogues of the peptide cross-bridges in peptidoglycan
  • Therefore, they can preferentially bind to the transpeptidase enzymes (one of the penicillin binding proteins PBPs)
  • This stops transpeptidation, so the peptidoglycan cannot form
  • BACTERICIDAL
  • More effective against Gram +ve bacteria as target more accessible
  • Resistance seen in some bacteria through beta-lactamases
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6
Q

What is the action and some features of chloroquine?

A
  • Antimalarial, both prophylactic and therapeutic.
  • In schizogony in erythrocytes, Plasmodium must degrade haemoglobin for its own use, in an acid vesicle.
  • Chloroquine concentrates in this vesicle and prevents crystallisation of toxic haem to nontoxic haemozoin; also binds to haem to form highly toxic FP-chloroquine.
  • Causes cell lysis and parasite autodigestion.
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7
Q

What is the action and some features of chlorpheniramine?

A
  • First-generation antihistamine, H1 antagonist. Aka chlorphenamine.
  • Inhibits type I hypersensitivity reactions. Usually used for mild allergic conditions such as allergic rhinitis (hayfever).
  • Side-effects: sleepiness, weakness, dry mouth.
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8
Q

What is the action and some features of ciprofloxacin?

A
  • Antibiotic of the fluoroquinolone class.
  • Binds to DNA gyrase, causing introduction of double-strand breaks in DNA.
  • They are BACTERICIDAL or BACTERIOSTATIC
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9
Q

What is the action and some features of cisplatin?

A
  • Alkylating agent used in cytotoxic chemotherapy.
  • Platinum bound to two NH3 and two Cl. Cl displaced by water, cross-links DNA bases.
  • Remarkably effective in testicular cancer, even metastatic.
    • Increased cure rate from 10% to 80%
  • Displacement of the chlorine allows cross-linking of the DNA strands
    • This leads to cytotoxicity
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10
Q

What is the action and some features of cromoglicate?

A
  • Described as a mast cell stabiliser, inhibits degranulation.
  • Used to prevent type I hypersensitivity reactions, as chronic prophylaxis in asthma.
    • Long-term treatment
  • Largely replaced by leukotriene receptor antagonists due to their convenience - cromoglicate must be taken 4 times a day.
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11
Q

What is the action and some features of cyclophosphamide?

A
  • Alkylating agent used in cytotoxic chemotherapy.
  • Chloride atoms displaced to crosslink nitrogens of guanine bases.
  • In vivo it is oxidised to phosphoramide mustard
  • The chlorines can take part in displacement reaction, which cross-link the DNA strands and can induce damage
  • It is effective in treating cancer and other conditions (e.g. rheumatoid arthritis)
  • Selectivity is determined by:
    • The aldophosphamide intermediate is detoxified by aldehyde dehydrogenase (ALDH)
    • This confers some selectivity for cells with low ALDH
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12
Q

What is the action and some features of dexamethasone?

A
  • Steroid - synthetic glucocorticoid.
  • Acts at nuclear glucocorticoid receptors, reduces phospholipase A2 synthesis. Reduces synthesis of lipid mediators of inflammation - prostaglandins, leukotrienes, platelet activating factor. Reduces inflammation and oedema.
  • Prostaglandins sensitise C-fibre pain neurons, so reduces inflammatory pain. Analgesic.
  • Side-effects:
    • Immune depression, susceptibility to infection
    • Hypertension - action at mineralocorticoid receptor, sodium/fluid retention
    • Bone resorption, diabetes, peptic ulcers, impaired skin healing
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13
Q

What is the action and some features of doxorubicin?

A
  • Aka Adriamycin
  • Used as cytotoxic chemotherapy.
  • Very planar and intercalates between base pairs.
  • Stabilises DNA topoisomerase II at reaction intermediate with double-strand breaks.
  • Prevents detangling of sister chromatids and induces double-strand breaks.
  • Topoisomerase is expressed most during G2 of the cell cycle.
  • This means that the cells in this phase are most susceptible to doxorubicin
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14
Q

What is the action and some features of erythromycin?

A
  • Antibiotic of the macrolide class.
  • Acts at ribosomal 50s subunit to inhibit translocation of tRNA, preventing protein synthesis
  • They are BACTERICIDAL/BACTERIOSTATIC
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15
Q

What is the action and some features of flucloxacillin?

A
  • Type of penicillin
  • β-lactam antibiotic.
  • Binds to and inhibits penicillin-binding proteins (PBP) - transpeptidases involved in peptidoglycan synthesis.
  • They are structural analogues of the peptide cross-bridges in peptidoglycan
  • Therefore, they can preferentially bind to the transpeptidase enzymes (one of the penicillin binding proteins PBPs)
  • This stops transpeptidation, so the peptidoglycan cannot form
  • BACTERICIDAL
  • More effective against Gram +ve bacteria as target more accessible
  • Resistance seen in some bacteria through beta-lactamases
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16
Q

What is the action and some features of gentamicin?

A
  • Antibiotic of the aminoglycoside class.
  • Acts at 30s subunit to inhibit translation initiation, therefore also inhibiting protein synthesis.
  • Like all aminoglycosides, is ototoxic.
  • They are BACTERICIDAL
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17
Q

What is the action and some features of heparin?

A
  • Anticoagulant.
  • A long, unbranched polysaccharide chain composed of repeating disaccharide units.
  • Allosterically activates antithrombin-III; stabilises ATIII-thrombin interaction by 2000-4000x, promoting thrombin breakdown by this serpin.
  • ATIII (anti-thrombin III) is an endogenous inhibitor of coagulation factors, especially Factor Xa and Thrombin (IIa)
  • Heparin stabilises these interactions, slowing the clotting cascade
    • Therefore, it is useful for prevention and treatment of thrombosis
  • Active in minutes so given to reduce risk of clots in acute MI.
    • Given as IV bolus then subcutaneous
  • Can cause severe bleeding and Heparin-induced thrombocytopenia (low levels of platelets)
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18
Q

What is the action and some features of imatinib?

A
  • Aka Glivec
  • Targetted chemotherapy drug - small molecule inhibitors of cell cycle enzymes.
  • Small-molecule inhibitor of the tyrosine kinase product of the BCR-ABL fusion gene on the Philadelphia chromosome.
    • It is also effective against other tyrosine kinases, so it is effective against multiple types of cancer
  • Used to treat Philadelphia +ve cancers; almost all chronic myelogenous leukaemias, some chronic lymphoblastic leukaemias.
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19
Q

What is the action and some features of isonizid?

A
  • Antibiotic, specifically against mycobacteria.
  • Works by inhibiting synthesis of long-chain mycolic acids.
  • Bactericidal to growing organisms, otherwise bacteriostatic
20
Q

What is the action and some features of maraviroc?

A
  • Used to treat HIV.
  • Prevents entry by binding and blocking CCR5.
  • Fairly significant risk of hepatotoxicity.
21
Q

What is the action and some features of methotrexate?

A
  • Antimetabolite used as a cytotoxic chemotherapy agent.
  • Close analogue of folic acid - competitive inhibitor of DHFR.
    • This inhibits synthesis of purines and dTMP
    • Thus, this inhibits RNA synthesis and DNA replication
  • Also used as a first-line DMARD in rheumatoid arthritis.
22
Q

What is the action and some features of NSAIDs?

A
  • Class of drugs which inhibit COX. Inhibit synthesis of lipid mediators of inflammation - prostaglandins, leukotrienes, PAF. Reduce inflammation and oedema.
  • Prostaglandins sensitise C-fibre pain neurons, so NSAIDs reduce inflammatory pain.
23
Q

What is the action and some features of oseltamivir?

A
  • Aka Tamiflu
  • Antiviral used to treat influenza. Also can be preventative for those at high risk.
  • Competitive inhibitor of neuraminidase. Prevents cleavage of sialic acid residues so release of new virions.
24
Q

What is the action and some features of paracetamol?

A
  • Analgesic but not considered an NSAID as it doesn’t reduce inflammation. Also has antipyretic properties.
  • Appears to inhibit COX (according to spec, “a specific COX”) - action seems to come from inhibition of COX2 in the brain.
  • Its metabolite AM404 is a weak cannabinoid receptor agonist, which may also contribute to analgesia.
25
Q

What is the action and some features of penicillin?

A
  • β-lactam antibiotic.
  • Binds to and inhibits penicillin-binding proteins (PBP) - transpeptidases involved in peptidoglycan synthesis.
  • They are structural analogues of the peptide cross-bridges in peptidoglycan
  • Therefore, they can preferentially bind to the transpeptidase enzymes (one of the penicillin binding proteins PBPs)
  • This stops transpeptidation, so the peptidoglycan cannot form
  • BACTERICIDAL
  • More effective against Gram +ve bacteria as target more accessible
  • Resistance seen in some bacteria through beta-lactamases
26
Q

What is the action and some features of raltegravir?

A
  • Inhibits integrase. Used to treat HIV. May also be used as part of post-exposure prophylaxis.
  • Prevents integration of viral DNA into the human genome so transcription of viral mRNA.
27
Q

What is the action and some features of rifampicin?

A
  • Of the rifamycin class of antibiotics.
  • Inhibits bacterial RNA polymerase [DNA-dependent] so inhibits transcription.
  • Used particularly for TB.
  • They are BACTERICIDAL or BACTERIOSTATIC
28
Q

What is the action and some features of saquinavir?

A
  • HIV protease inhibitor, used to treat or prevent HIV.
  • Protease required for cleavage of HIV polyproteins to release functional HIV proteins.
29
Q

What is the action and some features of simvastatin?

A
  • Statin, so is a HMG-CoA reductase inhibitor.
  • Inhibits cholesterol biosynthesis, lowers plasma LDL.
  • They also increases hepatic LDL receptor expression
  • This leads to decreased plasma LDL and plasma triglycerides, as well as slightly increased plasma HDL
  • Reduces risk/slows progression of atherosclerosis and thus coronary heart disease.
30
Q

What is the action and some features of streptokinase?

A
  • Thrombolytic agent.
  • The enzyme of beta-haemolytic Streptococci - dissolves blood clots by converting plasminogen to plasmin.
  • Used in treatment of acute MI with aspirin.
  • However most individuals have anti-streptokinase antibodies. Not recommended to be used twice in a person’s lifetime.
  • Administration: IV infusion or via catheter at site of arterial blockage
  • Side-effects: increased risk of bleeding, nausea.
  • Contraindictions:
    • Recent Strep infection
    • Stroke
    • Pregnancy
31
Q

What is the action and some features of streptomycin?

A
  • Antibiotic of the aminoglycoside class.
  • Acts at 30s subunit to inhibit translation initiation and therefore prevents protein synthesis.
  • Like all aminoglycosides, is ototoxic.
  • BACTERICIDAL
32
Q

What is the action and some features of tamoxifen?

A
  • Hormonal therapy for breast cancer
  • Oestrogen receptor modulator.
  • In breast tissue, acts as an ER antagonist. Used to treat ER-positive breast cancer.
    • Thus, it stops the growth of breast cells
    • It is metabolised to hydroxytamoxifen
  • It may also have other unknown mechanisms of action
33
Q

What is the action and some features of tetracycline?

A
  • Antibiotic of the tetracycline class.
  • Acts at ribosomal 30s subunit to inhibit tRNA binding.
  • Inhibits protein synthesis
  • BACTERICIDAL
  • Can be exported by membrane pumps
  • [[spec incorrectly classifies this as an aminoglycoside, it acts at the same ribosomal subunit but is its own class]]
34
Q

What is the action and some features of trastuzumab?

A
  • Aka Herceptin
  • Anti-HER2/Neu monoclonal antibody.
  • Blocks the growth factor receptor HER2, inhibits neoplasia where growth is driven by its overexpression.
    • This down-regulates the growth factor signals that are mediated by the HER2 receptors and it also induces antibody-dependent cellular cytotoxicity (ADCC)
  • HER2+ breast cancer and HER2+ stomach cancer
35
Q

What is the action and some features of trimethoprim?

A
  • Antibiotic of the 2,4-diaminopyridine class.
  • Dihydrofolate reductase (DHFR) inhibitor - this converts dihydrofolate to tetrahydrofolate so inhibits nucleotide synthesis.
  • They are BACTERIOSTATIC (but bactericidal when combined with sulfonamides)
36
Q

What is the action and some features of vincristine?

A
  • Vinca alkaloid
  • Used as a cytotoxic chemotherapy agent.
  • Binds to tubulin and prevents polymerisation into microtubules, so prevents movement and separation of chromatids in metaphase and leads to apoptosis.
  • Side-effects: hair loss, change in sensation/neuropathic pain, difficulty walking, headaches.
  • Dangers of vinca alkaloids such as vincristine:
    • They are severely neurotoxic, since they inhibit microtubules, which are essential in neurons for neurotransmitter transport.
    • Therefore they cannot be administered into the CSF, but must be administered via IV
37
Q

What is the action and some features of warfarin?

A
  • Vitamin K epoxide reductase inhibitor.
  • This re-reduces oxidised vitamin K to reduced vitamin K. Requires oxidation of NADH.
    • In coagulation factors, the glutamic acid residues must be gamma carboxylated into order to bind calcium, which is necessary for formation of complexes with platelet surfaces.
    • This gamma carboxylation is dependent on vitamin K.
  • Reduced Vitamin K is a cofactor for factors 2, 7, 9 and 10 (2 is thrombin) - anticoagulant.
  • Used for prophylaxis/treatment of:
    • DVT, pulmonary embolism
    • Thrombosis after heart valve replacement or MI/AF
  • Problems:
    • Narrow therapeutic window
    • Risk of haemorrhage
    • Many drug-drug interactions as it binds to albumin in plasma
  • Contraindictions - pregnancy, alcoholism
38
Q

What is the action and some features of zanamivir?

A
  • Aka Relenza
  • Antiviral used to treat influenza. Also can be preventative for those at high risk.
  • Competitive inhibitor of neuraminidase. Prevents cleavage of sialic acid residues so release of new virions.
39
Q

What is the action and some features of zidovudine?

A
  • Aka Azidothymidine/AZT
  • Of the chain terminator class of RT inibitors. Also known as nucleoside RT inhibitors.
  • Thymidine analogue that prevents DNA chain extension.
  • Used for treatment and prevention of HIV, prevents viral replication.
40
Q

What is the action and some features of abatacept?

[EXTRA]

A
  • Fusion protein - extracellular portion of CTLA-4 fused to human IgG Fc region.
  • CTLA-4 binds to B7 on activated APCs, higher-affinity competitive inhibitor of CD28 binding and T-cell activation. Costimulation blockade.
  • Unclear whether Fc portion actually does anything, I think it’s just to make it soluble (as CTLA-4 is a transmembrane protein). Davis et al 2007 - weakly binds to FcR but doesn’t cause ADCC.
  • Rheumatoid arthritis
41
Q

What is the action and some features of amantadine?

[EXTRA]

A
  • M2 ion channel inhibitor, used to treat influenza A virus.
  • Not often used for influenza A due to widespread resistance.
  • (Also, used in combination with L-DOPA for Parkinson’s dyskinesia. Weak NMDA antagonist, increased DA release and inhibits uptake.)
42
Q

What is the action and some features of apixaban?

[EXTRA]

A
  • New anticoagulant.
  • Highly selective factor Xa inhibitor, required for conversion of prothrombin to thrombin.
  • Side-effects: nausea, greatly increased risk of bleeding.
43
Q

What is the action and some features of ezetimibe?

[EXTRA]

A
  • Inhibits absorption of dietary cholesterol
  • Used to lower plasma cholesterol.
44
Q

What is the action and some features of ganciclovir?

[EXTRA]

A
  • Guanosine analogue. Converted by viral thymidine kinase (but not human thymidine kinase) to aciclovir triphosphate, which inhibits DNA polymerase in infected cells.
  • Used against HHV-5 (cytomegalovirus) herpesvirus.
45
Q

What is the action and some features of interferon alpha?

[EXTRA]

A
  • Used to treat chronic Hepatitis C infections.
  • Now largely replaced by more targetted treatments due to common adverse side effects eg. fever, headache, fever, arthralgia and myalgia.
46
Q

What is the action and some features of rituximab?

[EXTRA]

A
  • Anti-CD20 antibody.
  • Causes B-cell apoptosis, complement-mediated lysis and antibody-dependent cytotoxicity ( ADCC ).
  • Depletes B-cells in the hope non self-reactive or cancerous cells will repopulate.
  • Rheumatoid arthritis, chronic lymphocytic leukaemia, non-Hodgkin’s lymphoma
47
Q
A

YEAR 2 - Principles of Pathology (18 decks)

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