204 Core Drugs Flashcards
Core Drug : NSAIDs
Mechanism?
Indication?
Side effects?
Non-opioid analgesics
The main mechanism of action of NSAIDs is the inhibition of the enzyme cyclooxygenase (COX)
Used for mild to moderate pain and in inflammatory conditions
Side effects - GI toxicity - irritation, ulcers, bleeding, colitis, upper GI bleeding, nephrotoxicity
Core Drug : Aspirin Drug class? Mechanism? Indication? Side effects?
NSAIDS
Use for pain and inflammation limited by
- GI toxicity
- Tinnitus – mechanism obscure, usually reversible
- Reye’s syndrome (fulminant hepatic failure in children)
Anti-platelet effect
- Primary and secondary prevention eg stroke and MI
- Treatment of acute MI and stroke
Core Drug : Ibuprofen Drug class? Mechanism? Indication? Side effects?
NSAIDs
Ibuprofen available over the counter is demonstrably the least associated with side-effects
but can include - Irritation
Ulcers (gastric 15-30%, duodenal 10%)
Bleeding, Colitis, upper GI bleeding
Used for mild to moderate pain and inflammation
Core Drug : Ciclosporin Drug class? Mechanism? Indication? Main toxicities?
Ciclosporin belongs to a group of medicines called immunosuppressants - DMARDs
Inhibits calcineurin, which in turn reduces T lymphocyte activity
Similar indications to aza/ metho, but used more in Dermatology and transplantation
Main toxicities
- Nephrotoxic
- Hepatotoxic
- Gum hyperplasia
- Hirsuitism
Note tacrolimus (newer formulation) is easier to take, and available for topical use (esp eczema)
Core Drug : Azathioprine Drug class? Mechanism? Indication? what upset is very common?
Azathioprine is a type of medicine called an immunosuppressant (DMARD).
Inhibits thiopurine S methyltransferase (TPMT), so also inhibits purine synthesis
Similar indications to methotrexate; more widely used in transplantation compared to methotrexate
Toxicities similar to methotrexate; GI upset very common when starting
Core Drug: Methotrexate Drug class? Mechanism? Indication? Side effects?
Methotrexate belongs to the class of chemotherapy drugs called antimetabolites. (DMARDs)
Competitive inhibitor of dihydrofolate reductase (DHR), therefore anti-folate action
Folate needed for purine synthesis in DNA
This reduces T cell activity, and also (in higher doses) tumour synthesis
Main indications
Rheumatoid arthritis
Psoriasis
Crohns disease
Main toxicities
Hepatotoxicity
Leucopenia
Pulmonary fibrosis
Teratogenic
NOTE weekly dosing; errors have caused major toxicity
What DMARD has weekly dosing?
Methotrexate - NOTE weekly dosing; errors have caused major toxicity
Core Drug: Infliximab
Drug class?
Mechanism?
Indication?
TNF blocker - Infliximab – partially humanized mouse monoclonal anti-hTNF-a antibody
Used for Rheumatoid arthritis
NICE only approves infliximab, if combined with MTX
- Combined with MTX, they give excellent joint protection
Also used for the treatment of Crohn’s disease, ulcerative colitis, plaque psoriasis, ankylosing spondylitis
First choice DMARD, the gold standard
Methotrexate
Side effects of DMARDs
Nausea Loss of appetite Diarrhoea Rash, allergic reactions Headache Hair loss Risk of infections (pneumonia) Hepatotoxicity (metabolism) Kidney toxicity (route of elimination)
The TNF-blockers
- combined with … they give excellent joint protection
Combined with MTX, they give excellent joint protection
Core Drug: Rituximab
Drug class?
Mechanism?
Indication?
Partially humanized anti-CD20 mAb - Rituximab opsonized B-cells are attacked and killed by three mechanisms:
1)Complement mediated cytotoxicity
2-3) Antibody-dependent cell mediated cytotoxicity (ADCC) – FcgR or CR mediated opsonic phagocytosis
4) Apoptosis
Treatment of Rheumatoid arthritis (Also used for the treatment of SLE) and some cancers
Core Drug: Allopurinol
Drug class?
Mechanism?
Indication?
Allopurinol is a medicine used to lower levels of uric acid in your blood
mainly used for the long-term treatment and prevention of gout
Core Drug: Colchicine
Drug class?
Mechanism?
Indication?
Colchicine is in a class of medications called anti-gout agents - used for an Acute gout attack Colchicine works by decreasing swelling and lessening the build up of uric acid crystals that cause pain in the affected joint(s)
acute gout attack drug vs long term?
Colchicine - acute gout attack
allopurinol - long term