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.
Diamorphine indications
severe surgery related pain, MI, Palliative pain, relief of dyspnoea in acute pulmonary oedema
Diamorphine drug class
Opioid analgesic
Dalteparin drug class
LMWH anticoagulant
Dalteparin indications
Treatment of DVT, PE, unstable coronary artery disease
Acute conditions e.g. cancer, bed rest, heart failure, severe lung disease
Dobutamine drug class
Beta-1 agonist (inotropic agent)
Indications for dobutamine
inotropic support (increase force of muscle contraction) in infarction, cardiac surgery, cardiomyopathies, septic shock, cardiogenic shock
cardiac stress testing
Side effects of dobutamine
Arrhythmias, bronchospasm, chest pain, dyspnoea, eosinophilia, fever, headache, IHD, nausea, palpitations, urinary urgency, vasoconstriction
Doxazosin drug class
Alpha blocker
Doxazosin indications
HTN, benign prostatic hyperplasia
Side effects of Doxazosin
Arrhythmias, chest pain, cough, dizziness
Ephedrine indications
Reversal of hypotension from spinal or epidural anaesthesia, revesible airwya obstruction, Neuropathic oedema, nasal congestion, sinusitis
Erythromycin drug class
Macrolide antibiotic
Erythromycin indications
Susceptible infections in patients with penicillin hypersensitivity, gram positive and atypical bacteria, community acquired pneumonia, sore throat, otitis media, uncomplicated chlamydia, chronic prostatitis
Furosemide drug class
Loop diuretic
Furosemide indications
Treatment of edema associated with congestive heart failure, cirrhosis of the liver, and renal disease, including the nephrotic syndrome, in adults and pediatric patients, resistant HTN
Furosemide mechanism of active
Furosemide, like other loop diuretics, acts by inhibiting the luminal Na-K-Cl cotransporter in the thick ascending limb of the loop of Henle, by binding to the chloride transport channel, thus causing more sodium, chloride, and potassium to be excreted in the urine.
Ipratropium Indications
anticholinergic drug used in the control of symptoms related to bronchospasm in chronic obstructive pulmonary disease (COPD), asthma exacerbation, severe or life-threatening acute asthma
Ipratropium class
antimuscarinic
Ipratropium mechanism of action
Ipratropium is an acetylcholine antagonist via blockade of muscarinic cholinergic receptors. Blocking cholinergic receptors decreases the production of cyclic guanosine monophosphate (cGMP). This decrease in the lung airways will lead to decreased contraction of the smooth muscles.
Loperamide indications
Acute diarrhoea, chronic diarrhoea, faecal incontinence
Loperamide mechanism of action
Loperamide binds to the opiate receptor in the gut wall. Consequently, it inhibits the release of acetylcholine and prostaglandins, thereby reducing propulsive peristalsis, and increasing intestinal transit time. Loperamide increases the tone of the anal sphincter, thereby reducing incontinence and urgency.
Metformin drug class
Biguanide
Metformin mechanism of action
Metformin exerts its effect mainly by decreasing gluconeogenesis and by increasing peripheral utilisation of glucose; since it acts only in the presence of endogenous insulin it is effective only if there are some residual functioning pancreatic islet cells.
Metformin indications
T2DM, PCOS
Methotrexate drug class
DMARD
Methotraxate mechanism of action
Methotrexate inhibits the enzyme dihydrofolate reductase, essential for the synthesis of purines and pyrimidines.
Indications for methotrexate
Severe Crohns, Maintenance of remission of Chrons, Moderate to severe RA, severe active RA, Neoplastic disease
Oxybutinin indications
Overactive bladder or symptoms of detrusor overactivity, including urinary frequency and urgency
Ramipril class
ACE inhibitor
Ramipril indications
HTN, Symptomatic heart failure, Prophylaxis following MI, prevention of cardiovascular events in patients at high risk, nephropathy
Ramipril mechanism of action
Ramipril inhibits angiotensin-converting enzyme and decreases angiotensin II formation. As a result, sympathetic activity goes down, sodium and water reabsorption from the kidneys reduces, smooth muscles in the arterioles also relax. As a result, blood pressure decreases
Rifampicin indications
Brucellosis, Legionnaires, serious staph infections, endocarditis in combination, TB in combination, Gram positive cocci (staph and strep), C.diff and select Gram negative pathogens e.g. Neiserria meningitides, N.gonorrhoeae and HiB
Rivaroxaban class
DOAC, Factor Xa inhibitor, anticoagulant
Rivaroxaban indications
Prophylaxis of venous thromboembolism, treatment of DVT or PE, Stroke Prophylaxis
DOAC mechanism of action
The mechanism of action of rivaroxaban and all other factor Xa inhibitors is the inhibition of prothrombinase complex-bound and clot-associated factor Xa, resulting in a reduction of the thrombin burst during the propagation phase of the coagulation cascade.
Salmeterol drug class
Long-acting beta-agonists (LABA)
LABA mechanism of action
LABAs activate pre-junctional β2-adrenoceptors and reduce acetylcholine release thereby prevent any functional competition by acetylcholine at post-junctional muscarinic receptors in the airways occupied by LAMAs
Salmeterol indications
Reversible airways obstruction in patients requiring long-term regular bronchodilator therapy,
Nocturnal asthma in patients requiring long-term regular bronchodilator therapy,
Prevention of exercise-induced bronchospasm in patients requiring long-term regular bronchodilator therapy,
Chronic asthma only in patients who regularly use an inhaled corticosteroid (not for immediate relief of acute asthma)
COPD
Side effects of LABA
Arrhythmias, headache, palpitation, tremor
Sildenafil indications
Pulmonary arterial hypertension, ED
Suxamethonium drug class
Neuromuscular blocker
Suxamethonium indications
Neuromuscular blockade during surgery
Tamsulosin indication
Benign prostatic hyperplasia
Tamsulosin class
alpha blocker
Tamsulosin mechanism of action
Tamsulosin is in a class of medications called alpha blockers. It works by relaxing the muscles in the prostate and bladder so that urine can flow easily
Tramadol class
Opiate analgesics
Tramadol indications
Moderate to severe pain, chronic pain, postoperative pain
Metyrapone indications
Cushings syndrome/disease - it reduces the production of cortisol by the adrenals
Propylthiouracil and Methimazole indications
PTU - Used in hyperthyroidism to reduce thryoid hormones
Clopidogrel class and indications
Anti-platelet medication
Indications: Prevent atherothrombotic events: in PCI (with aspirin), TIA, Peripheral arterial disease, Acute coronary syndrome without ST elevation, acute STEMI, A.fib with at least one rf for vascular event
Ticagrelor drug action/class
P2Y12 receptor antagonist that prevents ADP-mediated P2Y12 dependant platelet activation and aggregation
Ticagrelor indications
Preventing artherothrombotic events in patients with: acute coronary syndrome, history of MI
Name two fibrinolytic agent used in the management of STEMI
Streptokinase, Alteplase and Tenecteplase
Fondaparinux class and indications
Antithrombin therapy, used for the management of NSTEMI unless the patient has a high bleeding risk
What are the 6 A’s of secondary prevention of an Acute Coronary syndrome?
Aspirin
Another anti-platelet e.g. ticagrelor or clopidogrel
Atorvastatin
ACE inhibitor e.g. ramipril
Atenolol or another beta-blocker
Aldosterone antagonist for those with clinical heart failure (eplerenone)
Risks of using ACE inhibitor and aldosterone antagonists
Hyperkalaemia
Ticagrelor mechanism of action
Inhibits ADP binding to platelet receptors. Prevents activation of glycoprotein IIb/IIIA complex so ADP cannot bind which limits platelet aggregation
Aspirin mechanism of action
irreversibly binding to COX, an enzyme that converts arachidonic acid to prostaglandin – one of these is Thromboxane A2 which facilitate platelet aggregation
DOAC mechanism of action
Directly inhibit clotting factor Xa
Warfarin mechanism of action
Inhibits production of Vit K dependant clotting factors (2,7,9,10)
Dabigatran Mechanism of action
Thrombin inhibitor
Why can beta blockers worsen peripheral artery disease
Beta-blockers should be avoided in peripheral artery disease as they can restrict blood flow to peripheral blood vessels, by blocking beta-adrenergic receptors, hence worsening oxygen delivery
Mechanism of action of thiazide like diuretics
Thiazides/thiazide-like drugs (e.g. indapamide) - inhibits sodium reabsorption by blocking the Na+-Cl− symporter at the beginning of the distal convoluted tubule
Hydroxycarbamide indications and action
Sickle cell anaemia
Stimulated production of HbF which has a protective effect against sickle cell crises and acute chest syndrome
Hydroxyurea indications and action
Prophylaxis for painful episodes in sickle cell anaemia, causes increased HbF
