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All drugs Flashcards

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1
Q

What are the contraindications to ACE inhibitors and ARBs?

A

Pregnancy Hyperkalaemia Bilateral renal artery stenosis *Change to ARB if angioedema

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2
Q

What are some of the dihydropyridine calcium channel blockers?

A

Amlodipine Lercanidipine Nifedipine Felodipine

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3
Q

What are the contraindications for calcium channel blockers?

A

Heart failure 2nd or 3rd degree heart block Tachyarhythmia (dihydropyridine)

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4
Q

What drugs are used for alzheimers?

A

Donepezil - anticholinesterase, increased vagal tone Galantamine - anticholinesterase, renal and hepatic clearance Rivastigmine - anticholinesterase, patch Memantine - NMDA antagonist, CI in seizures

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5
Q

What is pentoxifylline?

A

Pentoxifylline is a xanthine derivative which acts as a vasodilator and decreases blood viscosity.

Used in peripheral vascular disease.

Side effects - flushing, headaches, angina, arrhythmias, aseptic meningitis.

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6
Q

What is the MOA and use of acetazolamide?

A

Carbonic anhydrase inhibitor

Used in idiopathic intracranial hypertension

Glaucoma (open and closed angle)

Epilepsy

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7
Q

What is the MOA of topiramate?

A

An antiepileptic which blocks voltage gated Na channels and enhances GABA. Has some carbonic anhydrase activity.

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8
Q

What is pizotifen (MOA, use, risks)

A

It is a serotonin antagonist, weak anti-histamine, and anticholindergic

Use in migraine prophylaxis

Risks: weight gain, anticholinergic side effects, seizures, sedation

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9
Q

What is 5-ASA (MOA, use, risks)

A

These are immunomodulatory drugs including sulfasalazine, mesalazine, olsalazine and balsalazide. MOA is unknown

Used in UC, rarely Crohns

Well tolerated with minimal risks or side effects

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10
Q

What is cyclosporin (MOA, use, risks)

A

A calcineurin inhibitor in T cells which inhibits transcription of IL-2 and other pro-inflammatory cytokines this leads to decreased T cell proliferation and cell mediated immunity.

Used in transplants, nephrotic syndromes, many inflammatory conditions

Risks - nephrotoxic, HTN, neurotoxicity(tremor, myopathy), infections, HUS, hypomagnesaemia, diabetes

** Measure a 2 hour level

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11
Q

What is azathioprine and mercaptopurine (MOA, use, risks)

A

These are purine antimetabolites. AZA is the pro-drug of 6-MP. Are metabolised to 6-thioguanine (6-TGN), this is influenced by TPMT and XO

Used in a wide variety of inflammatory conditions notably IBD, trasplant

Risks: alterations in metabolism, bone marrow supression, infection, allopecia, GI upset, hepatitis, hypersensitivity syndrome

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12
Q

What are the risks of dopamine agonists?

A

Ergot derived (bromocriptine and carbergoline) can cause fibrosis eg retroperitoneal fibrosis

Impulsive behaviour

Can worsen restless legs paradoxically

Hallucinations and confusion

Sudden sleep onset

Orthostatic hypotension

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13
Q

What is pirfenidone (MOA, use, risks)

A

An anti-fibrotic used in idiopathic pulmonary fibrosis. It has been shown to regulate activity of TGF ß1 and TGFa, inhibits fibroblast proliferation and collegen synthesis.

Used in IPF (cannot have FVC<50% or DLCO <30%)

Risks - photosensitivity, nausea, rash, diarrhoea

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14
Q

What is nintedanib (MOA, use, risks)

A

A mutli-target tyrosine kinase inhibitor which sows proliferation of fibroblasts

Used - IPF (FVC >50% and DLCO >30%)

Risk - GI upset, diarrhoea nausea

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15
Q

What are the PDE5 inhibitors? (MOA, use, risk)

A

Sildenafil

Tadalafil

Inhibit PDE5 which leads to increased NO concentration and vasodilation

Use: Pulmonary HTN

Risks: pulmonary oedema, CYP34A, sickle cell disease, nose bleeds, hypotension, headache

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16
Q

What is methotrexate (MOA, use, risks)

A

Folic acid antagonist. Inhibits DNA synthesis and cell replication. Immunomodulatory - unclear MOA

Used: multiple malignancy, multiple autoimmune conditions including RA

Risks: teratogenic, GI upset, hair loss, hepatotoxicity, interstitial lung disease, ulcers

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17
Q

What is leflunomide (MOA, use, risks)

A

Inhibits dihydro-orotate dehydrogenase which leads to inhibition of pyrimidine synthesis in leukocytes and other rapidly dividing cells. Also has a uricosuric effect

Use: RA, psoriatic arthritis

Risks: lymphoproliferative disease, cytopenia, SJS/TENS, interstitial lung disease, LFT derrangement, GI upset, peripheral neuropathy

** has extensive entero-hepatic circulation so needs cholestyramine for washout

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18
Q

What is hydroxychloroqunine (MOA, use, risks)

A

An immunomodulator unclear MOA

Use: SLE, RA, malaria

Risks: retinopathy, myelosupression, worsening of psoriasis, ototoxicity, hyperpigmentation, rash

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19
Q

What is mycophenolate (MOA, use, risks)

A

Inhibits inosine monophosphate dehydrogenase which leads to depletion of guanosine nucleotides which is required for purine synthesis.

Use: transplant immunosuppression, lupus nephritis

Risks: GI upset, infection, cytopenia, GI haemorrhage, GI perforation, pancreatitis, hepatitis

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20
Q

What are the endothelian receptor antagonists? (MOA, use, risks)

A

Bosentan

Macicentan

Ambrisentan

Endothelin antagonists block endothelin receptors, causing vasodilation and improving exercise capacity.

Use: Pulmonary HTN

Risks: hepatitis, oedema, hypersensitivity, palpitations, hypotension, anaemia, teratogenic

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21
Q

What are the prostacycline analogues? (MOA, use, risk)

A

Eprostanol

Iloprost

Beraprost

Trepostanol

Selexipag - receptor agonist

Cause direct vasodilation of pulmonary vasculature and inhibit platelet aggregation

Use: Pul HTN, severe raynauds

Risks: headahces, diarhoea, muscle cramps, bleeding, hypotension

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22
Q

What is venetoclax (MOA, use, risks)

A

Inhibits BCL-2 - an anti-apoptotic protein

Use: CLL

Risk: tumour lysis syndrome

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23
Q

What is gefitinib (MOA, use, risks)

A

A TKI EGFR inhibitor

Use: NSCLC which is EGFR positive

Risks: acneform rash, GI upset, haemorrhage, ILD, keratitis, hepatitis, pancreatitis

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24
Q

What are tolvapatan and conivaptan (MOA, use, risks)

A

These are vassopressin receptor antagonists used for euvolaemic hyponatraemia (SIADH)

Risks: thirst, hypovolaemia, uncontrolled correction of Na, hepatitis

Short term solution only

Na returns to pre-treatment levels when ceased

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25
What is Pegvisomat (MOA, use, risks)
A growth hormone recpetor antagonist Used in refractory cases of acromegaly Risks: hepatitis, injecion site reactions
26
What is pasireotide (MOA, use, risks)
A somatostatin receptor agonist, multireceptor Use: 2nd line medical therapy for acromegaly Risk: hyperglcaemia, diabetes, drug interactions
27
What is tacrolimus (MOA, use, risk)
A calcineurin inhibitor in T cells which inhibits transcription of IL-2 and other pro-inflammatory cytokines this leads to decreased T cell proliferation and cell mediated immunity. Used in transplants, nephrotic syndromes, many inflammatory conditions Risks - nephrotoxic, HTN, neurotoxicity(tremor, myopathy), infections, HUS, hypomagnesaemia, diabetes \*\* trough level measured
28
What is mycophenolate (MOA, use, risk)
A reversible inhibitor of IMPDH in purine biosynthesis leading to decreased lymphocyte proliferation/activation. It leads to G1 cycle arrest Mycophenolate mofetil is a prodrug of mycophenolate acid Use: immunosupression, transplant Risks: bone marrow suppression, GI upset, infection
29
What is sirolimus (MOA, use, risk)
Other name rapomycin. An mTOR inhibitor it binds to FKBP in T cells which prevents the cell from responding to signalling eg from IL-2. This leads to cell cycle arrest in G1. Use: some malignancies, transplant immunosuppresion Risks: cytopenias, thrombosis, oedema, hyperlipidaemia, diabetes, proteinuria, decreased wound healing, nephortoxicity
30
What is everolimus (MOA, use, risk)
An mTOR inhibitor it binds to FKBP in T cells which prevents the cell from responding to signalling eg from IL-2. This leads to cell cycle arrest in G1. Use: some malignancies, transplant immunosuppresion Risks: cytopenias, thrombosis, oedema, hyperlipidaemia, diabetes, proteinuria, decreased wound healing, nephortoxicity \*\* better bioavailability than sirolimus
31
What is belatacept (MOA, use, risk)
A CTLA4-Ig fusion protein which binds to the cosimulatory ligands (CD80 and CD86) to interupt their binding to CD28 on T cells. This leads to T cell anergy and apoptosis. Use: transplant immunosuppression Risks: cannot be used if EBV positive due to risks of EBV post transplant lymphoproliferative disease
32
What is phenytoin (MOA, use, risks)? What is its CYP450 effect?
Blocks voltaged gates and use dependant Na channels Good for partial seizures Risks: neurotoxicity, severe skin reactions (esp asian HLA-B1502), gingival hypertrophy, hirsutism, hepatotoxicity, diabetes, osteomalacia CYP450 - enzyme inducer
33
What is carbamazepine (MOA, use, risks)? What is its CYP450 effect?
Blocks voltage gated and use dependant Na channels. Good for partial seizures Risks: skin reactions (HLA-B1502), neurotoxicity, GI upset, agranulocytosis, aplastic anaemia, SIADH, psychiatric disorders, osteomalacia CYP450 inducer
34
What is gabapentin (MOA, use, risks)
Binds to alpha-2 delta protein subunit of high threshold voltage-dependent calcium channels, reducing calcium influx and neurotransmitter release Good for focal seizures, pain management, Risks: neurotoxicity, periperhal oedema, psychosis, respiratory depression
35
What is pregabalin (MOA, use, risks)
Binds to alpha-2 delta protein subunit of high threshold voltage-dependent calcium channels, reducing calcium influx and neurotransmitter release Used in partial seizures, pain management Risks: neurotoxicity, anti-cholinergic symptoms, depression, agitation, periperhal oedema, hypersensitivity, neutropenia, pancreatitis
36
What is ethosuxamide (MOA, use, risks)
Reduces low threshold voltage-dependent calcium conductance in thalamic neurones Used for absence seizures Risks: GI upset, psych, cytopenias, hypersensitivity
37
What is lacosamide (MOA, use, risks)
Enhances slow inactivation of voltage dependant sodium channels. Used for partial seizures Risks: prolonged PR interval (HB, bradycardia), neurotoxicity, hypersensitivity
38
What is valproate (MOA, use, risks)? What is its effects on CYP450?
Multiple mechanisms. Prevents repetitive neuronal discharge by blocking voltage‑ and use-dependent sodium channels. Other actions include enhancement of GABA, inhibition of glutamate and blockade of T-type calcium channels. Used for generalised and partial seziures, bipolar, migraine Risks: hepatotoxicity, hyperandrogenism, teratogenic, pancreatitis, cytopenias, hypersensitivity, osteoporosis Enzyme inhibitor of CYP450
39
What is lamotragine (MOA, use, risks)
Blocks voltage gated and use dependant Na channels and glutamate release Used for generalised seizures esp women of childbearing age. Bipolar Risks: neurotoxicity, alopecia, severe skin reactions, cytopenias
40
What is levetiracetam (MOA, use, risks)
Likely MOA by binding to SV2A and AMPa Used in gerneralised seizures Risks: psych, skin reactions, neurotoxicity
41
What is perampanel (MOA, use, risks)
A non-competative AMPa receptor blocker Used for generalised seizures Risks: psych, dizziness, somnolence, weight gain
42
What are the interferons for MS? (MOA, use, risks, effectiveness)
Immunoregulatory, increases suppression, reduces T cell proliferation Used in relapsing remitting MS, CIS Risks: flu like symptoms, depression Effect - Reduces relapses by 30%
43
What is glatiramer acetate? (MOA, use, risks, effectiveness)
Synthetic polyeptide which may block myelin presentation to T cells Use: Relapsing remiting MS, CIS Risks: post-injection reactions (palpitations, flushing) \* Safe in pregnancy Effect: 30% reduction relapses
44
What is teriflunomide? (MOA, use, risks, effectiveness)
Metabolite of leflunomide. Inhibits dihydroorotate dehydrogenase which is required for pyrimidine synthesis. Use: relapsing remitting MS Risks: GI upset, peripheral neuropathy, alopecia, LFT derrangement Effect: 30% reduction relapses \*\* not safe in pregnancy, needs cholestyramine washout
45
What is dimethyl fumarate? (MOA, use, risks, effectiveness)
Immunomodulator ?Nrf2 antioxidant pathway Use: relapsing remitting MS Risk: GI upset, flushing, lymphopenia, PML, proteinuria Effect: 50% reduction in relapses
46
What is fingolimod? (MOA, use, risks, effectiveness)
SIP agonist, reduces lymphocytes leaving lymph nodes Use: any relapsing MS Risks: transient bradycardia with first dose, HTN, LFT derrangemnt, macular oedema, infection, skin cancers, shingles Effect: 50% reduction in relpases
47
What is natalizumab? (MOA, use, risks, effectiveness)
Anti-alpha 4 integrin. Inhibits leukocyte migraton into the CNS Use: relpasing remitting MS Risks: PML, LFT derrangement, infusion reactions Effect: 68% reduction in relapses
48
What are the types of adverse drug reactions?
Type A - predictable, dose dependant. Common Type B - idiosyncratic, rare and often seen in post-marketing studies. Not predictable.
49
What are the properties of 1st order kinetics?
Rate of elimination depends on drug concentration There is exponential decay Cpss is reached in 4-5 half lives Steady state is altered by dosing and dosing interval Most drugs fall into this catagory
50
What are the properties of zero order kinetics?
Occur when a metabolic pathway is saturatable eg ETOH, aspirin, phenytoin Elimination is not related to concentration Change in dose leads to disproportiate changes in plasma concentrations
51
How is extraction ratio related to blood flow?
Extraction ratio is the amount of drug cleared in 1 passage across the liver. If it approaches 1 then almost all the drug is cleared and it is highly dependant on blood flow If it approaches 0 then minimal drug is cleared and it is more dependant on the liver function/enzymes
52
What are the 2 phases of hepatic drug clearence?
Phase 1 is oxidation, reduction, hydrolysis. Primarily performed by CYP enzymes Phase 2 is conjugations performed by transferases Both aim to make a drug more water soluble (polar) \*\*1st pass metabolism also performed by liver but this related to bioavailability rather than clearence
53
How does volume of distrbution affect 1/2 life?
The greater the Vd the longer the 1/2 life
54
What are the classes of drugs in pregnancy?
A - safe, good data B - 3 subcatagories, limited data, safe in animals, appears safe in humans C - Suspected of causing harm D - known to cause harm X - known to have a very high risk of permanent damage
55
What is the division between SJS and TENs?
SJS \<10% body surface area Overlap 10-30% TENs \>30%
56
What is the mechanism of action of acamprosate?
NMDA receptor and GABA A modulator Used for ETOH addiction
57
What is the mechanism of action of varenicline?
Partial agonist of nicotinic a4b2 receptor Used for smoking cessation
58
What is riluzole? (MOA, use, risks)
A sodium channel blocker which also inhibits glutamate release Used in ALS - improves survival by 2-3 months Risks: GI upset, dizziness, pancreatitis, interstitial lung disease, neutropenia
59
What is bortezomib? (MOA, use, risks)
A proteosome inhibitor leading to apoptosis. It prevents NFkB from entering the nucleus. Use: myeloma upfront treatment, maintanence, post-relapse Risks: peripheral neuropathy, hypotension, thrombocytopenia
60
What is carfilzomib? (MOA, use, risks)
Selective, reversible proteasome inhibitor. Causes apoptosis. Use: relapsed myeloma Risks: heart failure, hypertension, thromboyctopenia, VTE
61
What is erlotinib? (MOA, use, risks)
A first generation reversible EGFR inhibtor Used for EGFR mutant NSCLC (not T790M) Risks: acneform rash, pneumonitis, GI upset
62
What are the EGFR inhibitors used in lung cancer?
Erlotinib, gefitinib and afatinib are 1st line Osimertinib for relapse

Pharmacology (4 decks)

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