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MODA Drug Flashcards > Immunosuppressives > Flashcards

Immunosuppressives Flashcards

1
Q

Adalimumab

A

Human antibody that sequesters TNFα

Used in rheumatoid arthritis

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2
Q

Adrenaline

A

Administered intramuscularly/intravenously to counteract systemic vasodilatation and reduction in tissue perfusion in case of anaphylactic shock

Also relieves bronchospasm

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3
Q

Alemtuzumab

A

Humanised monoclonal antibody

Binds to CD52, antigen on mature lymphocytes, and targets these for destruction (but not stem cells from which they divide)

Causes destruction of T and B cells

Administered several times a week

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4
Q

Anakinra

A

Recombinant version of the IL-1 receptor antagonist

Binds to the IL-1R with a higher affinity than IL-1 itself, but does not initiate receptor signalling

Used in rheumatoid arthritis

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5
Q

Arthrotec

A

Combination of misoprostol and diclofenac

Used in chronic treatment of rheumatoid arthritis to prevent peptic ulcer formation

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6
Q

Aspirin

A

Acetylates serine at position 530, which irreversibly inhibits COX

Irreversible NSAID so has long-lasting actions

Production of ATL may contribute to the anti-inflammatory actions of aspirin

Also lowers the risk of platelet aggregation

Can trigger bronchospasm

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7
Q

Azathioprine

A

Inhibits de novo purine synthesis

In cells lacking a nucleotide salvage pathway (B- and T-cells)

Prodrug for 6-mercaptopurine (6-MP)

Converted by hypoxanthine phosphoribosyl transferase (HPRT) to thioinosic monophosphate (TIMP)

Used to diminish transplant rejection.

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8
Q

Basiliximab

A

Monoclonal antibody against the CD25 alpha subunit of the IL-2 receptor

IL-2 receptor antagonist

Decreases the incidence and severity of acute rejection following transplantation

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9
Q

Botulinum toxin A

A

Administered by intramuscular injection to head and neck

Treatment of serious migraines - 15+days/month

Migraine relief may be due to decreased release of neurotransmitters from nociceptors

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10
Q

Ciclosporin A

A

Isolated from the fungus Tolypocladium inflatum

Cyclic, 11 amino acid peptide

Binds to cyclophillin (CpN - a cytoplasmic protein) and inhibits IL-2 transcription via inhibition of calcineurin

Prevents T cell proliferation

Immunosuppressant

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11
Q

Cyclophosphamide

A

Alkylating agent

Prodrug

Converted by P450 enzymes in the liver first to aldophosphamide and then the active agent phosphoramide mustard

Cross links guanine in DNA via N7 groups

Immunosuppressive effect is due to killing of dividing T and B cells

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12
Q

Dexamethasone

A

Synthetic corticosteroid

Binds to glucocorticoid receptors

Used as anti-inflammatory and in immunosuppression

Half life >48 hours - long-acting

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13
Q

Ergotamine

A

Non-selective 5-HT1 partial agonist

Causes vasoconstriction

Inhibits nociceptor activity

Used to treat acute migraines

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14
Q

Etanercept

A

Fusion protein of the soluble TNFα receptor and the Fc portion of IgG1

Mops up the high levels of TNFα that occur in rheumatoid arthritis

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15
Q

Etoricoxib

A

NSAID

COX-2 selective inhibitor

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16
Q

Hydroxychloroquine

A

Usually used to treat malaria

Also administered to patients refractory to other DMARDs

Lipophilic weak base so accumulates in cytoplasmic acidic vesicles

Reduces antigen presentation by macrophages and reactive oxide species generation in neutrophils

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17
Q

Ibuprofen

A

NSAID

Non-selective COX inhibitor

Used as analgesic, antipyretic and anti-inflammatory

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18
Q

Icatibant

A

Selective bradykinin B2 antagonist

Prevents nociceptor activation and reduces pain

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19
Q

Imatinib

A

Receptor tyrosine kinase inhibitor

Used to treat mastocytosis

Only efficacious in patients NOT presenting with the common D816V c-Kit mutation

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20
Q

Loratadine

A

Selectively peripheral histamine H1-blocker

Non-drowsy as does not cross blood brain barrier

No cardiac side effects

Used to treat hay fever and urticaria

21
Q

Mepyramine

A

First generation antihistamine, targeting the H1 receptor

Causes drowsiness as crosses blood brain barrier

22
Q

Methotrexate

A

Folic acid antagonist

Dihydrofolate reductase inhibitor

Treatment of rheumatoid arthritis

Inhibits purine nucleotide and thymidylate synthesis and thus is anti-proliferative

23
Q

Misoprostol

A

Synthetic prostaglandin E 1 (PGE1) analogue

Decreases gastric acid secretion and increases mucin secretion

Administered with NSAIDs in patients at risk of developing gastric ulcers

24
Q

Naproxcinod

A

Combination of naproxen (NSAID) and NO donor

Not approved because side effects not better than currently-approved drugs

25
Naproxen
NSAID Non-selective COX inhibitor Small and enters the hydrophobic tunnels of both COX-1 and COX-2
26
Omalizumab
Humanised monoclonal Ab against IgE Binds to the Cε3 region of IgE Prevents IgE binding to FcεRI Reduces FcεRI expression and inhibits allergen induced mast cell degranulation Used in severe, persistent allergic asthma that are refractory to treatment
27
Omeprazole
Proton pump inhibitor Blocks H+-K+-ATPase Used to treat peptic ulcers
28
Ondansetron
Anti-emetic 5-HT3 receptor antagonist Used to treat chemotherapy-induced nausea and vomiting (CINV)
29
Paracetamol
Inhibits both COX-1 and COX-2 Some COX-2 selectivity through reduction of the site in COX enzymes required for the production of PGH2 from PGG2 Eliminated mainly through conjugation Overdose leads to major hepato- and renal toxicity Alcohol increases risk of toxicity due to upregulation of Cyp2E1
30
Penicillamine
Hydrolysis product of penicillin D-isomer can be used to treat rheumatoid arthritis May act by decreasing IL-1 and collagen synthesis Highly reactive thiol group
31
Prednisolone
Synthetic glucocorticoid Synthesis of anti-inflammatory proteins Blocks the transcription of inflammatory genes
32
Proglumide
CCK2 receptor antagonist Inhibits histamine release from ECL cells
33
Propranolol
Non-selective β adrenoreceptor antagonist
34
Ranitidine
Histamine H2-receptor antagonist Decreases proton excretion into stomach Used in the treatment of peptic ulcers
35
Rituximab
Monoclonal antibody, targeting CD20 that is primarily expressed by B cells Used in the treatment of moderate rheumatoid arthritis
36
Rofecoxib
COX-2 inhibitor Increased myocardial risk Withdrawn from market in 2004
37
Salbutamol
β2-adrenoreceptor agonist Short- acting drug taken as needed to control symptoms of asthma
38
Salmeterol
Long-acting β2-adrenoreceptor agonist Long, lipophilic tail enables it to be incorporated into the plasma membrane Used prophylactically in the treatment of asthma
39
Sirolimus
Macrolide antibiotic Binds to FKBP Sirolimus-FKBP complex binds to and inhibits mammalian target of rapamycin (mTOR) Results in decreased T cell activation and proliferation and a decreased immune response
40
Sodium aurothiomalate
Gold compound Used to treat rheumatoid arthritis Unknown mechanism Long term use can cause chrysiasis
41
Sodium cromoglycate
Mast cell “stabiliser” Inhibits degranulation Inhibits an inward Cl- conductance that is required to maintain a negative enough membrane potential to enable sustained influxes of extracellular calcium Stabilises plasma membrane and blocks release of mediators
42
Sulfasalazine
Broken down by colonic bacteria to produce sulfapyridine (a sulphonamide) and 5- aminosalicylic acid (a salicylate) 5-aminosalicylic acid scavenges reactive oxygen species released from neutrophils Used to treat rheumatoid arthritis
43
Sumatriptan
5-HT1B/D/F agonist Action at 5-HT1B causes vasoconstriction and 5-HT1D/F agonism inhibits nociceptor activity Used in acute migraine attacks
44
Tacrolimus
Macrolide antibiotic Binds to an immunophilin called FK-binding protein (FKBP) Inhibits CaN and IL-2 synthesis is inhibited Used to suppress the rejection of transplanted organs
45
Theophylline
PDE inhibitor producing increased cAMP Induces bronchodilation/mast cell stabilisation Used prophylactically in treatment of asthma
46
Trastuzumab
Herceptin Used to treat HER2 positive breast cancers
47
Zafirlukast
CysLT1 receptor antagonist Induces bronchodilation Used in treatment of asthma
48
Zileuton
5-LO inhibitor Can be used prophylactically as an extended release formula Inhibits leukotriene formation Prophylactic asthma treatment

MODA Drug Flashcards (7 decks)

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