Pharmacology Flashcards
Name three Bisphosphonate drugs
Alendronate, Pamidronate, Zoledronate
What are Bisphosphonates, calcitonin, SERM’s and denosumab useful in the treatment of?
Osteoporosis and Pagets
Mechanism of action of bisphosphonates
Inhibit bone resorption -> modest increase in bone mineral density and decreased fracture risk. Osteoclasts bind to bisphosphonates inhibiting their adherence to the bony surface. They decrease development and recruitment of osteoclast precursors and induce osteoclast apoptosis
What do bisphosphonates bind to in the bone?
Hydroxyapatite
Other indications for Alendronate
Useful in the treatment of hypercalcaemia
Side effects of bisphosphonates such as Alendronate
Upper GI side effects (E.g. acid reflux, Esophagitis and Esophageal uclers)
Osteonecrosis of the jaw
Hypocalcaemia
Explain the RANK-RANKL system
PTH stimulates osteoblasts to express RANKL and then RANKL binds to RANK on osteoclast to increase their activity
Class and Mechanism of action of denosumab
Monoclonal antibody against RANKL to inhibit osteoclast activity
Mechanism of action of calcitonin
Tones down calcium by inhibiting osteoclast activity to decrease bone resorption. It increases renal excretion of Calcium
Side effects of Calcitonin
Hypocalcaemia
What is atenolol indicated for?
Hypetension, Angina and Arrhythmias
What class of drugs does atenolol fall under?
Beta blocker
Name another drug in the same class as atenolol
Propanolol
Contraindications for atenolol (and all other beta blockers)
Asthma, hypotension, Bradycardia, metabolic acidosis, phaeochromocytoma, second and third degree AV block
Side effects of beta blockers
Abdominal discomfort, bradycardia, confusion, depression, diarrhoea, dizziness, nausea, fatigue, headache, syncope, sleep disturbance
Mechanism of action of beta blockers
Beta blockers, also called beta adrenergic blocking agents, block the release of the stress hormones adrenaline and noradrenaline in certain parts of the body. This results in a slowing of the heart rate and reduces the force at which blood is pumped around your body
Indications for Atracurium
Adjunct to general anaesthesia during surgery to relax skeletal muscle and to facilitate endotracheal intubation and mechanical ventilation
Atracurium mechanism of action
Atracurium antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate
Indications for Bendroflumethiazide
It’s used to treat high blood pressure (hypertension) and the build-up of fluid in your body (oedema)
Bendroflumethiazide class
Thiazide diuretic
Bendroflumethiazide mechanism of action
As a diuretic, bendroflumethiazide inhibits active chloride reabsorption at the early distal tubule via the Na-Cl cotransporter, resulting in an increase in the excretion of sodium, chloride, and water. Thiazides like bendroflumethiazide also inhibit sodium ion transport across the renal tubular epithelium through binding to the thiazide sensitive sodium-chloride transporter. This results in an increase in potassium excretion via the sodium-potassium exchange mechanism. The antihypertensive mechanism of bendroflumethiazide is less well understood although it may be mediated through its action on carbonic anhydrases in the smooth muscle or through its action on the large-conductance calcium-activated potassium (KCa) channel, also found in the smooth muscle.
Cefuroxime indications
Susceptible gram postitive and gram negative bacteria, acute diverticulitis, prophylaxis sometimes, LUT infection, acute pyelonephritis
Cefuroxime drug class
Cephalosporin antibiotic
Cefuroxime mechanism of action
Attach to penicillin binding proteins to interrupt cell wall biosynthesis, leading to bacterial cell lysis and death
Side effects of cephalosporins
Abdo pain, diarrhoea, dizziness, eosinophilia, leucopenia, neutropenia, thrombocytopenia, vomiting, vulvovaginal candidiasis
Celecoxib indications
Pain and inflammation in osteoarthritis, pain and inflammation in RA, ankylosing spondylitis
Contra-indications for Celecoxib
GI bleeding, ulceration, IBD, IHD
Celecoxib drug class
COX-2 inhibitor NSAID
Mechanism of action of Celecoxib
The mechanism of action of celecoxib is due to selective inhibition of cyclooxygenase-2 (COX-2), which is responsible for prostaglandin synthesis, an integral part of the pain and inflammation pathway. This pharmacologic activity gives celecoxib its analgesic, anti-inflammatory, and antipyretic effects.
Chloramphenicol indications
Superifical eye infections, Bacterial infection in otitis externa, HiB infections
Chloramphenicol drug class and action
Chloramphenicol is an antibiotic and is in the class of antimicrobials that inhibits protein synthesis.
Ciclosporin indications
Severe acute UC refractory to corticosteroid treatment, severe active RA, Nephrotic syndrome
Ciclosporin drug class
Disease-modifying anti-rheumatic drug or DMARD
Ciclosporin mechanism of action
Cyclosporine is a calcineurin inhibitor that inhibits T cell activation.
Other examples of DMARDs
Methotrexate, sulfasalazine, hydroxychloroquine and leflunomide
DMARD side effects
loss of appetite, nausea, diarrhoea, abdo pain, liver problems, increased infection risk
Ciprofloxacin indications
Bacterial eye infection, otitis externa, diabetic foot, acute diverticulitis (with metronidazole), resp infections, UTI, prostatitis, uncomplicated gonorrhoea, pyelonephritis
Ciprofloxacin drug class
Fluoroquinolone antibiotic
Side effects of quinolone antibiotics
Decreased appetite, arthralgia, constipation, diarrhoea, dizziness, dyspnoea, fever, fungal infection, GI discomfort, myalgia, headache, QT interval prolongation
Co-amoxiclav indications
Infections due to beta-lactamase-producing strains where amoxicillin is inappropriate, acute diverticulitis, diabetic foot, surgical prophylaxis, community-acquired pneumonia, hospital-acquired pneumonia, otitis media, pyelonephritis, UTI from catheter, osteomyelitis
Exacerbation of: bronchiectasis, COPD, sinusitis
Co-amoxiclav class
Penicillin
General mechanism of action for penicillins
Penicillin kills bacteria through binding of the beta-lactam ring to DD-transpeptidase, inhibiting its cross-linking activity and preventing new cell wall formation. Without a cell wall, a bacterial cell is vulnerable to outside water and molecular pressures, which causes the cell to quickly die.