Shared Flashcard Set

Details

Pharmacological agents
-
86
Medical
Undergraduate 1
03/14/2017

Additional Medical Flashcards

 


 

Cards

Term

Acetazolamide 

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Reversible carbonic anhydrase inhibitor 
  2. Uses in glaucoma, odema (drug and cardiac induced), epilepsy, high altitude sickness (acute),  and reducing intraocular pressure
  3. Action as a diuretic - prevents the conversion of carbonic acid into water and carbon dioxide, and therefore allows dissociation in tubule to bicarbonate and a hydrogen ion. The hydrogen ion can be recovered in exchange for sodium (NHE) which sets an osmotic gradient into the kidney tubule, thus reducing ECV. As a treatment of mountain sickness, the acid load counteracts the alkalosis brought on through increased respiration and thus allowing the chemoreceptors to respond to hypoxic stimuli.
  4. Side effects - acidosis, fatigue, tingling. Contraindications - hypokalaemia/natremia, kidney failure, acidosis
Term

 Aciclovir 

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antiviral
  2. Used for the treatment of herpes simplex, chicken pox, shingles as well as for the prevention of CMV following transplant and complications of EBV infection
  3. Converted by viral thymidine kinase to aciclovir monophosphate, then into aciclovir triphosphate which completely inactivates HSV-specific DNA polymerases by mimicking GTP. 
  4. Nausea, vomiting, diarrhea (systemic), burning, skin damage (topical)
Term

Adrenaline

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Endogenous hormone/neurotransmitter
  2. Anaphylaxis, cardiac arrest, superficial bleeding, asthma
  3. Broad spectrum effect by acting on adrenergic receptors. Higher affinity (compared to NAd) to α2, βand therefore effect on NAd release inhibition and smooth muscle relaxation (e.g. bronchodilation, dilation of SM in skeletal muscle arterioles). NA = NAd at β1 receptor, thus increasing cardiac output by increase in ino- and chronotropy. Na < NAd at α1, thus smaller effect in vasoconstriction within GI system, skin and kidneys
  4. Side effects - tachycardia, paleness, headache, anxiety, shakiness, nausea, sweating, angina, arrythmia, aortic rupture, cerebral haemorrhage. Contraindications - hypersenstivity to symapathomimetics, non-anaphylactic shock patients, in cases where vasopressor drugs are contraindicated (diabetes, preeclampsia), myocardial ischaemia, and CV disorders
Term

Amantadine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antiviral and antiparkinsonian
  2. Treatment of parkinson's disease, use in treatment of influenza (no longer recommended as 100% of seasonal pandemic influenza viruses resistant)
  3. Parkinson's disease - broad effects on dopaminergic, noradrenergic and serotongeric pathways (noradrenaline and dopamine release) as well as acting as a weak antagonist of NMDA-Rs. Psychostimulant effect through agonism of σreceptors (thought to modulate CNS calcium release from ER, and therefore increase dopaminergic transmission). Influenza - pore blockade of viral protein proton channel M2 which, in normal function, transports protons from the hosts intracellular acidified vacuoles to the virion interior and therefore allowing dissociation of ribonuceoproteins and viral replication. 
  4. Side effects generally concern the CNS - onset of nervousness, anxiety, agitation, insomnia and exacerbation of seizure disorders and psychiatric symptoms
Term

Aminophylline 

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Methyl xanthine derivative 
  2. Treatment of airway obstruction from asthma or COPD
  3. Competitve, nonselective phosphodiesterase inhibitor and therefore raises [cAMP]i, activates PKA while inhibiting TNF-α, leukotriene synthesis and a reduction of inflammation. Secondly, it acts as a nonselective adenosine receptor antagonist. Bronchodilation, diuresis (neurogenic), CNS and cardiac stimulation and gastric acid secretion by increasing cAMP production and therefore induction of adrenaline release
  4. Theophylline toxicity - seizure, hypotension and significant dysrhythmias 
Term

Amitriptyline 

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Tricyclic antidepressant 
  2. Major depressive and anxiety disorder, ADHD and bipolar disorderas well as the treatment of neuropathic pain 
  3. Strong antagonistic action on serotonin reuptake and moderate antagonist action on noradrenaline reuptake through interaction with the serotonin and noradrenaline transporters after metabolism to nortriptyline. Blockade of 5-HT-R and α1-R. Apparent agonist of TrkA and TrkB receptors (on which BDNF acts) - possible action for therapeutic efficacy as BDNF has powerful antidepressant effects
  4. Dizziness, headache, weight gain and some cognitive impairment (delirium and confusion) as well as negative interactions with MOA inhibitors, anticholinergic agents and antipsychotics. TCA overdose can result in convulsion, hypotension, stupor, coma and death. 
Term

Amlodipine 

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Calcium channel blocker
  2. Hypertension, angina and corony artery disease
  3. Angioselective blockade of calcium channels. Therefore calcium channels on vascular smooth muscle cells and cardiomyocytes can no longer facilitate as large an influx of calcium, reducing the contractility and reducing blood presure by increasing vessel diameter. Angina is relieved through the TPR and therefore the afterload, meaning the heart has to work less hard in systole (stable angina); blocks spasm of coronary arteries and returns proper blood flow to coronary arteries. Also evidence that amlodipine acts as an antimineralocorticoid. 
  4. Peripheral odema, dizziness, palpitations, and hypotension in overdose. Contraindications - shock or current hypotension through systemic vasodilation

 

Term

Amoxicillin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. β-lactam antibiotic
  2. Use in infection - specifically: bacterial sinusitis, commiunity acquired pneumonia, acne vulgaris, prophylaxis of bacterial endocarditis as well as otitis media, step. pharyngitis, UTIs, Salmonella, Lyme disease and chlamydia
  3. β-lactam antibiotic and therefore inhibits synthesis of bacterial cell walls by inhibition of cross linkage betweeen peptidoglycans (present in gram + and -, but gram - generally resistant)
  4. Nausea, vomiting and rash (both allergic and nonallergic)- occasionally severe anaphylaxis
Term

Aspirin

 (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. NSAID
  2. Analgesic for acute pain, control of febrile symptoms, anti-inflammatory agent, prophylaxis for high risk/secondary heart attacks and strokes 
  3. Irreversible inhibition of COX-1 (which acts to convert AA to produce precursors for prostaglandins, which themselves sensitise nociceptive neurons to stimuli) and modification of COX-2 activity (which normally acts to produce pro-inflammatory prostanoids, but when aspirin modified produced anti-inflammatory lipoxins). Aspirin irreversibly blocks the production of thromboxane A2 (COX1), thus inhibiting platelet aggregation 
  4. Contraindications - allergy to salicylates, peptic ulcer patients and haemophilia. Side effects - GI bleeds from peptic ulcers by increasing mucosal erosion, Reye's syndrome (encaphalopathy and fatty liver) in children and adolescents
Term

Atenolol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Beta blocker
  2. Hypertension, angina, long GT syndrome, acute MI, (supra)ventricular tachycardia, symptoms of alcohol withdrawal)
  3. Selective βreceptor anatagonist and therefore reduces sympathetic situmation. This reduces the cardiac workload, resting heart rate, cardiac output and mean arterial blood pressure without peripheral vasocontriction through action through βantagonism or negative inotropy
  4. Provocation of type 2 diabetes and weak protective action against MIs and stroke, overdose can cause shock, heart failure, hypoglycaemia and bronchospasm
Term

Atropine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Parasympatholytic
  2. Dilation of pupil for examination of glaucoma, treatment of bradycardia, inhibition of salivary and mucus secretion, organophosphate poisoning
  3. MAchR antagonism prevents parasympathetic tone in heart by acting on M2 to increase SA node firing and conduction through the AV node, secretions by acting on M1/3 and pupillary dilation by action on M3
  4. Ventricular fibrillation, tachycardia, dizziness, nausea, photophobia, dry mouth, dissociative hallucinations 
Term

Beclomethasone dipropionate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Steriod
  2. Long term asthma management, dermatitis, psoriasis, ulcerative colitis, allergic rhinitis
  3. Synthetic corticosteriod - bind to specific cytoplasmic receptors to reduce leukocyte infiltration and site of inflammation, interference with mediators in inflammatory response, suppresion of humeral immune responses and reduction in odema. Involvement of PA2 inhibitory proteins, lipocortins and downregulation of syntheisis of prostaglandins and leukotrienes 
  4. Respiratory infections, headache, throat inflammation, cataracts, Cushing syndrome and rare severe allergic reaction 
Term

Bendroflumethiazide

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Thiazide diuretic
  2. Mild heart failure, hypertension
  3. Blockade of Na+/Cl- symporter in the DCT of kidney inhibits sodium reabsorption and therefore increases sodium and water excretion from the kidney, reducing circulating volume
  4. Contraindications - hypotension, gout, renal failure, lithium therapy, hypokalaemia. Side effects - raise of uric acid levels in the blood, hypokalaemia (increased basolateral movement of Na/K exchanger and passive sodium loss, stimulationm of Na/K exchanger via increased aldosterone levels), hypercalcaemia (through overactivity of basolateral sodium-calcium antiporter)
Term

Benzylpenicillin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. β-lactam antibiotic
  2. Gram + antibacterial: use against pneumonia, strep throat, syphilis, necrotising enterocolitis, diptheria, gas gangrene, leptospriosis, cellulitis and second line agent against pneumococcal meningitis
  3. β-lactam - inhibition of formation of peptidoglycan cross links in bacterial cell walls by binding β-lactam ring to enzyme DD-transpeptidase, thus cross link formation cannot be catalysed
  4. Hypersensitivity reactions - urticaria, fever, joint pains, rashes, anaphylaxis and rare CNS toxicity convulsions
Term

Bupivicaine 

 (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Local anaesthetic
  2. Local surgery, peripheral nerve block, sympathetic nerve block, epidual/caudal block (use with adrenaline to vasoconstrict and and prevent systemic absorption/elongate duration of action)
  3. Bind to intracellular portion of voltage gated sodium channel - therefore preventing sodium influx into nerve cells and initiation of action potential and conduction of nociceptive signals
  4. Cardiotoxicity, systemic absorption can cause CV and CNS symptoms which lower [blood plasma], neuronal excitation followed by depression and coma. CV effects include CV collapse, hypotension, arrythmia, bradycardia and cardiac arrest 
Term

Buspirone

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. 5-HT1A receptor agonist
  2. Treatment of anxiety disorder (delayed onset) and possible augmentation of SSRIs in depression 
  3. Agonism of 5-HT1A receptor which are inhibitory autoreceptors and therefore causes a dose dependent reduction in serotonin levels, while increasing dopamine and NAd. Secondarily, low affinity block of D2 autoreceptor, and therefore increase in nigrostriatal dopamine release 
  4. Extensive list of side effects - most common include dizziness, headache, somnolence (drowziness) as well as altered mental state (attention deficit, depression, confusion, anger, co-ordination deficit, increased anxiety)
Term

Carbamazepine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Anti-convulsive, anti-psychotic
  2. Treatment of epilepsy, neuropathic pain, schizophrenia, bipolar disorder
  3. Use dependant blockade of voltage-gated sodium channels. Ionisation of carbamazepine within intracellular fluid allows binding to VG sodium channels and prevention of repetitive an sustained neuronal firing. Secondarily a GABA receptor agonist, and therefore potentiates GABA receptors which may contribute to efficacy in neuropathic pain and bipolar disorder. Some evidence as SRI
  4. Rare major aplastic anaemia and agranulocytotic effects, as well as increased suicide risk, increased hyponatraemia and ADH secretion, congenital malformation in foetus. Commonly causes drowsiness, dizziness, headaches, nausea, vomiting and enhanced CNS depression in combination with alcohol. 
Term

Chloroquine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antimalarial
  2. Treatment and prevention of malaria from vivax, ovale and malariae (widespread falciparum resistance)
  3. Within RBC, chloroquine is protonated and caps haemozoin molecule to prevent malarial biocrystallisation of heme (normally toxic heme is biocrystallised by malarial parasite to haemozoin) and leads to cell lysis and parasitic autodigestion
  4. Side effects include seizurees, GI reactions, headache, skin rashes and itchiness, metallic taste, retinopathy 
Term

Chlorpheniramine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antihistamine
  2. Prevention of allergic conditions such as rhinitis and urticaria
  3. H1 receptor antagonist - acts on mast cells, smooth muscle and endothelium to prevent effects of mast cell degranulation in allergic reaction - ileum contraction, itchin, vasodilatation, bronchoconstriction. Seems also to be a serotonin-NAd reuptake inhibitor and therefore possess antidepressant qualities
  4. Drowsiness (can cross BBB), dizziness, confusion, anxiety, nausea, dry mouth, hallucinations and irratibility
Term

Chlorpromazine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Typical antipsychotic
  2. Acute and chronic psychoses, schizophrenia, manic phase of bipolar and amphetamine-induced psychoses
  3. Strong antagonist of D2 receptor as well as D1 receptors therefore causing diminised neurotransmitter binding within forebrain. Dopamine receptor blockade - mesolimbic system for antipsychotic, nigrostriatal causes extrapyramidal effects, serotonin 1 and 2 receptor blockade causes antiaggressive and anxiolytic properties
  4. Tardive dyskinesia, akathisia (inner restlessness), weight gain, sedation, Parkinsonism, hypotension and dizziness. Contraindications include CNS depression, drug intoxication and liver disease/failure
Term

Ciprofloxacin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Broad spectrum antibiotic
  2. Treatment of bone and joint infections, intra-abdominal infections, infectious diarrhea, RTIs, skin infections, typhoid fever, UTIs, endocarditis, prostatitis, anthrax and chancroid.
  3. Broad spectrum antibiotic - action against both gram +/- bacteria through the inhibition of bacterial DNA gyrase (gram -) and type II topoisomerase (gram +), which inhibits the fission of bacterial cells during division
  4. Risk of tendinitis and tendon rupture, insomnia, restlessness, nausea, vomiting, diarrhea and headache. Enlongation of QT interval via blockage of VG potassium channels - can result in torsades de pointes (uncommon)
Term

Cisplatin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Chemotherapy medication
  2. Treatment of cancer including testicular, ovarian, breast, bladder, head and neck, cervical, lung, mesothelioma, eosophageal, brain and neuroblastoma
  3. Interference with DNA replication by displacement of chloride ligand by two guanine bases within DNA and forming crosslinkage. This, therefore, interferes with cell division and triggers apoptotic pathways through Omi/Htra2 mechanism. 
  4. Nephrotoxicity, neurotoxicity, nausea and vomiting, hearing loss, hypomagnesaemia, hypokalaemia and hypocalcaemia as well as haemolytic anaemia via haemolysis
Term

Clozapine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Atypical antipsychotic
  2. Treatment of schizophrenia
  3. Partial 5-HT2A antagonist (negative symptom eleviation), direct interaction with GABAB receptors as a positive allosteric modulator suggests role in reduction in locomotor changes, induction of glutamate and D-serine release as well blockade of dopamine receptors
  4. Constipation, bed wetting, stiffness, sedation, tremors, hypotension, weight gain, extrapyramidal symptoms, agranulocytosis, CNS depression, leuko/neutropenia
Term

Codeine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Opiate
  2. Analgesic, cough/diarrhea medication
  3. Conversion to morphine - Gi coupled receptors on nociceptive terminals reduce the release of substance P, GABA, dopamine, NAd and ACh as well as opening OP3 and OP1 channels resulting in hyperpolarisation and reduced neuronal excitability
  4. Drowsiness, constipation, itching, nausea, vomiting, dry mouth and potential respitory depression in overdose - cause of physical dependence and therefore opioid withdrawal symptoms
Term

Cromoglicate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)


Definition
  1. Mast cell stabiliser
  2. Asthma medication 
  3. Prevents release of chemoattractants and chemokines that attract inflammatory cells, as well as stabilising inflammatory cells. Thought to inhibit exaggerated neuronal reflexes triggered by irratant receptors on nerve endings, inhibit release of cytokines from T cells and eosinophils
  4. Angioedema, bronchospasm, cough, headache, pain, nausea, rash and swollen parotid glands (all uncommon)
Term

Cyclopentolate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

 
Definition
  1. Parasympatholytic
  2. Paediatric eye exams, reversal of CNS effects of nonspecific AChase block
  3. Blockade of local mAChR receptors, preventing accomodation of eye to different distances, which is normally mediated by parasympathetic, ACh pathways
  4. Disorientation, incoherent speech and visual disturbances
Term

Cyclophosphamide 

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

 
Definition
  1. Chemotherapy agent
  2. Lymphoma, multiple myeloma, leukemia, ovarian cancer, breast cancer, small cell lung cancer and sarcoma
  3. Active metaboltic phosphoramide mustard formed in cells with low levels of ALDH (aldehyde dehydrogenase). In these cells, phosphoramide mustard forms DNA corsslinks between DNA stands at guanine residues, leading to cell apoptosis via mitosis failure. Toxicity low as bone marrow stem cells, liver and intestinal epithelium contain high concentration of ALDH which converts phosphoramide mustard into non-toxic compound. Cyclophosphamide induces immunomodulatory effects in adaptive immunotherapy, which are thought to be brought about by elimation of Tregs and induction of T cell growth factors
  4. Nausea, vomiting, stomach ache, cystitis, hair loss, bladder bleeding, infection through neutropenia or lymphoma and premature menopause risk
Term

Dexamethasone

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

 
Definition
  1. Steroid
  2. Rheumatic problems, severe allergies, asthma, chronic obstructive lung disease, croup and brain swelling
  3. Corticosteriod - bind to specific cytoplasmic receptors to reduce leukocyte infiltration and site of inflammation, interference with mediators in inflammatory response, suppresion of humeral immune responses and reduction in odema. Involvement of PA2 inhibitory proteins, lipocortins and downregulation of syntheisis of prostaglandins and leukotrienes
  4. Acne, insomnia, vertigo, weight gain, impaired healing, depression, euphoria, hypertension, vomiting, cararacts, amnesia, irritability, malaise and headaches as well as withdrawal from long term treatment leading to hypotension, fever, adrenal insufficiency, weight loss and myalgia
Term

Diazepam

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

  

Definition
  • Benzodiazepine
  • Anxiety, seizures, neurovegetative symptoms of vertigo, withdrawal treatment (alcohol/opiate), insomnia, tetanus, hallucinogen or stimulant overdose/psychosis
  • Positive allosteric modulation of GABAA receptors (ligand gated chloride channels) allowing hyperpolarisation of neuron Em. Diazepam's action seems to be localised mainly to the limbic system, thalamus and hypothalamus - as well as the cerebral cortex. Anti-convulsant properties are thought to be due to the binding and slowing of recovery from inactivation of VG sodium channels.
  • Anterograde amnesia, confusion, ataxia, suppresion of REM and slow wave sleep, depression, as well as tolerance and dependence symptoms (which can be life threatening)
Term
Digoxin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

 

 
Definition
  1. Cardiac glycoside
  2. AF and atrial flutter, heart failure (not first line)
  3. Inhibition of the NA-K ATPase in myocardium increases intracellular Na levels, and thus runs down/reverses the Na-Ca exchanger and increases the [Ca2+]i. This then increases calcium storage in the SR and increases contractility during cross bridge cycling without an increased oxygen demand
  4. Narrow therapeutic window - loss of appeitite, nausea, vomiting, diarrhea, blurred vision, confusion, drowsinesss, dizziness, insomnia, agitation and depression. Less frequently - psychosis, delerium, amnesia, convulsions or heart block. 
Term

Doxazosin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

 

 
Definition
  1. α1 receptor antagonist
  2. Hypertension, urinary retention associated with benign prostate hyperplasia, PTSD treatment
  3. Blockade of αreceptors on vascular smooth muscle inhibits the vasoconstrictive action of noradrenaline, and therefore reduces blood pressure. Doxazosin is an inverse agonist as these receptors have tonic activity. 
  4. Dizziness, headache, drowsiness, lethargy, weakness, palpitations, nausea
Term

Doxorubicin

 (drug class, medical uses, mechanism of action, notable side effects/contraindications)

 

 
Definition
  1. Chemotherapy agent
  2. Some leukaemias, Hodgekin's lymphoma, bladder, breast, stomach, lung, ovaries, thyroid, soft tissue sarcoma, multiple myeloma
  3. Intercalation and inhibition of biosynthesis. Inhibits progression of topoisomerase II, which facilitates the relaxation of DNA supercoils for transcription. Doxorubicin stabilises the complex after the DNA has been broken down, thus preventing its reassembly and progression of replication. 
  4. Cardiomyopathy leading to congestive heart failure, thought to be through oxidative stress (release of quinone type free radicals), downregulation of contractile protein genes and p53 mediated apoptosis. Can result in typhlitis (infection of bowel) and chemotherapy induced acral erythema
Term

Erythromycin

 (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Bacteriostatic antibiotic
  2. Treatment of skin and URTIs caused by (but not confined to): Haemophilus influenzae, Staphylococcus aureus, Streptococcus pyogenes, Corynebacterium minutissimum
  3. Binding to 50s subunit of rRNA appears to inhibit translation of bacterial proteins. Interference with aminoacyl transferase to prevent transfer of tRNA to A site on rRNA complex and therefore preventing the expansion of the microbial protein
  4. Very common GI effects - diarrhea, nausea, abdominal pain and vomiting because erythromycin is a motilin agonist (therefore can be used to treat gastroparesis). Allergic reactions can be anaphylactic, while less common side effects include arrythmia and prolonged QT interval
Term

Flucloxacillin

  (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. β-lactam antibiotic
  2. Activity against β lactamase organisms such as Staph. aureus, unlike other β-lactam antibiotics. Treatment of chest, ear, nose, throat, skin and soft tissue infections as well as endocarditis, osteomyelitis, meningitis, enteritis, septicaemia and UTIs
  3. β-lactam antibiotic and therefore inhibits synthesis of bacterial cell walls by inhibition of cross linkage betweeen peptidoglycans (present in gram + and -, but gram - generally resistant). Presence of isoazolyl side chain facilitates β lactamase resistance through steric hinderance
  4. Diarrhea, nausea, urticaria, pain, inflammation, allergy and increase in liver enzymes.
Term

Fluoxetine

  (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. SSRI
  2. Depression, OCD, PTSD, bulimia nervosa, panic disorder, premenstrual dysphoric disorder and trichotillomania
  3. Delay of uptake of serotonin and therefore resulting in serotonin persisting in the synapse by acting as an antagonist to the SERT. Fluoxetine appears to have several other interactions in the CNS, such as increasing concentrations of allopregnanolone (GABA positive allosteric modulator), and σagonism, the clinical significance of which is not clear
  4. Abnormal dreams, abnormal ejaculation, anorexia, anxiety, diarrhea, nausea, anxiety, sweating, tremor, sexual dysfunction, increased suicide risk and risk of overdose. Contraindications include MOAI, NSAIDS (synagistic blood thinning effect) and other serotonergic drugs
Term

Furosemide

  (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Loop diuretic
  2. Hypertension, odema from congestive heart failure, odema from hepatic cirrhosis, renal impairment, nephrotic syndrome and management of severe hypercalcemia
  3. Inhibition of NKCC2 pump, preventing the uptake of sodium, potassium and two chloride ions into the cell, and thus increasing the amount of active osmolytes in the kidney filtrate. 
  4. Can result in possible ototoxicity, hyperglycaemia, hyperuricaemia and hypokalaemia (use in combination with amiloride)Potential negative interactions with a wide range of other drugs including analgesics, antibiotics, antidepressants, antiepileptics, antihypertensives etc. which exaccerbate side effects of furosemide.
Term

Gentamicin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Bactericidal antibiotic
  2. Wide range of bacterial infections, mainly gram -. Pseudomonas, Proteus, E. coli, Klebsiella pneumoniae, Enterobacter aerogenes causing RTIs, UTIs, blood, bone and soft tissue infections.
  3. Irreversible binding to 30S subunit of ribosome, interrupting protein synthesis. 
  4. Nausea, vomiting, low blood count, allergic response, neuromuscular problems, nerve damage, nephrotoxicity and ototoxicity
Term

Glyceryl Trinitrate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Nitrate
  2. Angina pectoris from ischaemic heart disease, antihypertensive
  3. Metabolite is NO, which activates guanylyl cyclase to activate cGMP from GTP. cGMP activates myosin light chain phosphatase via cGMP dependent kinase to prevent further contraction. At low doses, dilatation of veins to reduce preload and therefore workload of the heart (and oxygen demand). This also decreases the compression of coronary arteries and allows coronary blood flow. At high doses, vasodilatation of the arteries occurs, reducing afterload and further decreasing the heart's workload. 
  4. Orthostatic hypotension, severe headaches, bradycardia. Contraindication s- other vasodilator drugs such as those used for erectile dysfunction (sildenafil)
Term

Glycopyrrolate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. mAChR antagonist
  2. Reduction of salivary, tracheobronchial, pharyngeal and the acidity of gastric secretions during surgery. Use in conjunction with neostigmine to prevent overactivity of mAChR during NMJ blockade. Can be used in stomach ulcer treatment to reduce gastric secretion
  3. Blockade of mAChR, thus lowering muscarinic-mediated parasympathetic tone.
  4. Reduction in sweating, hyperthermia, dry mouth, headaches, diarrhea, constipation and drowsiness
Term

Haloperidol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Typical antipsychotic
  2. Schizophrenia, acute psychosis (drug/fever induced), hyperactivity, delirium, alcohol or opium withdrawal, neurological tic or Tourette disorders, BPD
  3. High affinity D2 antagonism with slow dissociation. Binds also to α1 receptors at low dose, and 5-HT2 receptors at high dose. The lack of affinity for histamine or muscarinic receptors results in lower incidence of sedation, weight gain, hypotension but increases rates of extrapyramidal systems
  4. Extrapyramidal symptoms - dystonia, akathisia, bradykinesia, temor, parkinsonism as well as hypotension and somnolence
Term

Heparin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Endogenous anticoagulant
  2. Acute corony syndrome (including non-STEMI), AF, DVT, PEs, cardiopulmonary bypass, haemofiltration and indwelling catheters
  3. Binds to enzyme inhibitor antithrombin III, causing an conformational change to an active form. AT then inactivates thrombin, factor Xa and other proteases at a 1000-fold increased rate. As inhibition of thrombin requires 18 saccharide units for formation, while Xa only requires a pentasaccharide binding site, the development of LMW heparins has lead to a compound that will specifically bind and inhibit factor Xa resulting in a wider therapeutic window and greater subtlety of coagulation regulation
  4. Heparin induced thrombocytopenia through platelet degredation by immune system, elevation of aminotransferase levels, hyperkalaemia as a result of aldosterone suppresion. Chronic use can result in alopecia and osteoporosis. Contraindications - severe hypertension, severe liver disease and haemophilia
Term

Ibuprofen

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. NSAID
  2. Fever, pain, menstruation, osteoarthritis, headaches and kidney stone pain. Inflammatory disease treatment including juvenile idiopathic arthritis and RA.
  3. Non selective COX inhibitor to prevent conversion of AA to prostaglandin H2, which is in turn converted to other prostaglandins and thromboxane A2. COX-2 appears to connot analgesic, antipyretic and anti-inflammatory effects. Antipyretic effects may be due to action of hypothalamus resulting in increased blood flow, vasodilation and thus heat dissapation. 
  4. Nausea, dyspepsia, diarrhea, constipation, GI bleeding and ulceration, fluid retention and hypertension. Contraindications with alcohol consumption on gastric ulceration. Overdose can lead to GI bleeds, seizures, coma, acute renal failure, respitory depression and cardiac arrest
Term

Imatinib

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Chemotherapy agent
  2. Chronic myelogenous leukemia, GI stromal tumours, Philadelphia chromosome+ acute lymphocytic leukemia, systemic mastocytosis and myelodysplastic syndrome
  3. Specific inhibitor of tyrosine kinase enzymes by the occupation of TK active site. Specific for TK domain in abl, c-kit and PDGF-R. In the Philedelpia chromosome, there is a fusion of abl and bcr leading to bcr-abl fusion protein, which is a constituetively active tyrosine kinase, the activity of which is reduced by imatinib. Bcr-abl activates proliferation pathways such as Ras/MapK and JAK/STAT, as well as pathways involved in reduced adhesion such as Src/Pax/Fak/Rac. Inhibition of bcr-abl stimulates its entry into the nucleus, where it cannot perform normal anti-apoptotic functions and thus resulting in tumour cell death.
  4. Nausea, diarrhea, headaches, cramps, fluid retention, bleeding, weight gain, neutro/thrombocytopenia, anaemia, cardiotoxicity can result in congestive heart failure
Term

Ipratropium

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Non-specific mAChR antagonist
  2. COPD, minor bronchial asthma prevention
  3. Block of mAChR promotes degredation of intercallular cGMP which in turn decreases contractility of smooth muscle in the lung - increasing bronchodilation and reducing mucus secretion. 
  4. Rare effects as local effect - can cause dry mouth, sedation, skin flusing, tachycardia, nausea, palpitations, headache. Contraindication for prostatic hypertrophy for use as nebuliser, as urinary retention has been observed. 
Term

Isoflurane

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. General anaesthetic
  2. In conjunction with air and nitrous oxide as a rapid anaesthetic inducer (although generally used to maintain anaesthesia after it has been induced by agents such as thiopentone or propofol)
  3. Mechanism of action not fully understood. Reduction of pain sensitivity and muscle relaxant effects likely caused by binding to GABA, glutamate and glycine receptors to different degrees. Potentiation of glycine receptor activity reduces motor function, inhibition of NMDA receptors and inhibits conduction in activated potassium channels. Activation of calcium ATPase by increasing membrane fluidity. 
  4. Postoperative cognitive dysfunction in elderly, possible neurodegeneration when used in children. Irratation of respiratory system during anaesthesia induction (thus not widely used for induction)
Term

L-dopa

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Endogenous dopamine precursor
  2. Treatment of Parkinson's disease and dopamine-responsive dystonia
  3. L-dopa can enter the BBB, where it is converted to dopamine by DOPA decarboxylase. Administration must be carried out with a peripheral DOPA decarboxylase inhibitor such as carbidopa to prevent the peripheral effects of excess dopamine and other monoamine formation and transmission
  4. Hypotension, arrythmia, nausea, disturbed respiration, hair loss, confusion, anxiety, auditory hallucinations, resistance, dyskinesia as end-of-dose deterioration of function.
Term

Lidocaine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Local anaesthetic
  2. Local numbing agent and heart arrhythmia
  3. Blockade of fast voltage gated sodium channels within the neuronal membrane to prevent nociceptive signal propagation, while in the heart the blockade raises the depolarisation threshold and therefore reduces the likelihood of early action potentials and arrythmia
  4. Rare for local anaesthetic, system exposure can cause CNS excitation or depression (dose dependent), cardiovascular arrest as well as usual allergic reaction symptoms. Absolute contraindications with any heart block syndrome
Term

Lithium

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antidepressant 
  2. Treatment of bipolar, major depression, schizophrenia
  3. Interaction with many neurotransmitters and receptors to decrease NAd and increase serotonin release. No obvious psychotropic effects. Possible interaction with NO signalling pathway, and therefore synaptic plasticity
  4. Common effects include confusion, memory deficit, diarrhea, dry mouth, tremor, EKG T wave changes, elevated white blood cell count, muscle weakness, polyuria and weight gain. Lithium competes for ADH receptors and therefore causes nephrogenic diabetes insipidus as well as hypothyroidism. Associated with kidney damage.
Term

Losartan

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antgiotensin II receptor antagonist
  2. Hypertension, delay progession of diabetic nephropathy,
  3. Selective, competitive antagonism of angiotensin II receptor type I (AT1). This decreases total peripheral resistance (afterload) and the venous return (preload). Also specific inhibitor of urate transporter 1 (URAT1) and thus prevents uric acid uptake and increases secretion. 
  4. Fetal toxicity, URIs, dizziness, congestion and back pain. Hypotension, hyperkalaemia and allergic reaction
Term

Methotrexate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Chemotherapy agent
  2. Treatment of breast, head and neck, leukaemia, lymphoma, lung, osteosarcoma, bladder and trophoblastic neoplasms. Also used for psoriasis, RA and Chron's disease. Can be used for pregnancy termination
  3. Antifolate type antimetabolite. Competetive inhibition of dihydrofolate reductase which normally converts dihydrofolate to tetrahydrofolate, which is needed for the de novo synthesis of thymidine. As well as this, folate is essential for the synthesis of purines and pyramidines. In RA, methotrexate appears to inhibit T cell activation, downregulate B cellsand inhibit IL-1β binding. 
  4. Hepatoxicity, ulcerative stomatitis, leukopenia, nausea, abdominal pain, fatigue, fever, dizziness and acute pneumonitis. Penicillin may prevent elimination of methotrexate and therefore increasing toxicity
Term

Morphine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Opiate analgesic
  2. Pain (myocardial infaction and labour), shortness of breath, opioid use disorder
  3. Interaction predominantly with the μ-opioid receptor of the CNS and GI tract. These receptors act to produce analgesia and sedation within the amygdala, hypothalamus, thalamus, caudate nucleus, putamen and laminae I and II of spinal cord. 
  4. Causes constipation by preventing propulsive peristalsis, hypogonadism, CNS depression, negative inpact on anterograde and retrograde memory as well as addiction and severe symptoms of physical withdrawal - anxiety, irritability, depression, dysphoria, restless leg syndrome, tachycardia, vomiting, diarrhea. 
Term

Naloxone

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. μ-opioid receptor inverse agonist
  2. Opioid overdose and prevention of opioid abuse
  3. μ-opioid receptor blockade as a competitive antagonist produces rapid onset of withdrawal symptoms
  4. Little or no effect without presence of opioids - when opioids present can result in sweating, nausea, restlessness, trembling, vomiting, flushing, headache and possible arrythmia. Appears to be capable of blocking the placebo pain lowering response
Term

Neostigmine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. AChE inhibition
  2. Myasthenia gravis, reversal of effects of non-depolarising muscle relaxants (vecuronium), treatment of acute colonic pseudo-obstruction and delay of effects of envenomation from snakebite
  3. Prevention of breakdown of ACh increases ACh levels in nAChR and mAChR synapses, but does not cross BBB or placenta. 
  4. Headache, brow pain, blurred vision, phacodonesis, congestive iritis, allergic reactions, bradycardia (thus usually given with atropine), nausea, abdominal cramps and diarrhea
Term

Nicotine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Parasympathomimetic stimulant
  2. Increase in cognition, alertness and focus. As treatment for nicotine addiction.
  3. In CNS, bind to nAChRs to elicit psychoactive effects and increasing neurotransmitter release. Activates receptors on neurons that innervate VTA of mesolimbic pathway, and therefore cause dopamine release (reward pathway). Apparent induction of release of endogenous opioids to reinforce effects. Activates sympathetic nervous system by acting on sphlachnic nerves to adrenal medulla and releasing Ad.
  4. Association with inhalation of tobacco. Some evidence that nicotine acts as a tumour promotor. Most negative effects through withdrawal - irratability, anxiety, craving). Overdose possible but dose is unlikely in recreational use.
Term

Nifedipine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Calcium channel blocker
  2. Long term treatment of hypertension and angina pectoralis. Used as tocolytic in premature labour
  3. L-type calcium channel blockade, as well as non selective voltage gated calcium channel blockade. In vascular smooth muscle, with reduces the contraction of arteries and increases diameter, as well as reducing the force of contraction in the heart by limiting the influx of calcium ions. In the heart, calcium channel blockade slows conduction of electrical activity and therefore produces a negative chronotropic effect. Blockade of calcium channel signalling in the adrenal medulla reduces the aldosterone production, and therefore also contributes to reduction in hypertension. Reduction in afterload reduces heart workload and therefore limits the oxygen requirement and subsequently the angina pectoralis. 
  4. Dizziness, tachycardia, hypotension
Term

Odansetron

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antiemetic
  2. As a antiemetic in cancer treatment, postoperatively, in gastroenteritis and during pregnancy for morning sickness
  3. Highly specific and selcetive 5-HT3 receptor antagonist. These receptors are found peripherally on vagal terminals and in the central chemoreceptor trigger zone (area postrema). Serotonin is released by enterochromaffin cells in small intestine in resoinse ti chemotherapeutic agents which stimulates vagal afferents to induce vomiting. It is the antagonism of this reflex that appears to prevent vomiting.
  4. Usually well tolerated, but can result in constipation, diarrhea, dizziness, headache and may be associated with the prolongation of the OT interval and progression to torsades de pointes (therefore contraindications in patients with congenital long QT syndrome, congestive heart failure, and bradyarrhythmias)
Term

Paracetamol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Analgesic
  2. Reduction of fever and treatment of pain from osteoarthritis, lower back pain, headaches, postoperatively and in dental procedures (although NSAIDs may be more effective in some of these cases)
  3. Mechanism is not fully understood. Thought to be a COX-2 selective antagonist, and thus reduce the production of prostaglandins and therefore pain potentiation but, through the action of peroxides within inflammatory legions, have a negligible anti-inflammatory effect. Thought that paracetamol may suppress signal transduction through metabolite NAPQI acting on TRPA-1 receptors which transduce signals to superficial, nociceptive layers of the spinal cord. However, also postulated that NAPQI interacts with cysteine proteases that process procytokines such as IL-1 and IL-6 to give analgesic effects
  4. Tocixity as foremost case of acute liver failure so contraindications in chronic alcoholics and patients with liver damage. Skin reactions to paracetamol (SJS and toxic epidermal necrolysis) while overdose causes nausea, vomiting, sweating and acute liver failure.
Term

Penicillin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. β-lactam antibiotic
  2. Gram + antibacterial: use against pneumonia, strep throat, syphilis, necrotising enterocolitis, diptheria, gas gangrene, leptospriosis, cellulitis and second line agent against pneumococcal meningitis. NOTE - penicillin G is given intravenously (see benzylpenicillin) while penicillin V can be given orally as is more acid-stable but less active against gram negative bacteria
  3. β-lactam - inhibition of formation of peptidoglycan cross links in bacterial cell walls by binding β-lactam ring to enzyme DD-transpeptidase, thus cross link formation cannot be catalysed
  4. Hypersensitivity reactions - urticaria, fever, joint pains, rashes, anaphylaxis and rare CNS toxicity convulsions
Term

Phenelzine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antidepressant & anxiolytic
  2. Treatment of major depressive disorder, dysthymia, BD, panic disorder, social anxiety disorder, bulimia and PTSD
  3. Non selective and irreversible inhibitor of MAO-A and MAO-B. Therefore, breakdown of serotonin, melatonin, NAd, Ad and dopamine is inhibited. To a lesser extent, inhibition of alanine transaminase and GABA transaminase to increase alanine and GABA levels in brain. Requires several weeks to achieve full therapeutic effects and therefore thought to have further neuroadaptive effects on autoreceptors and enzyme expression
  4. Common side effects include dizziness, blurry vision, headache, lethargy, sedation, somnolence, insomnia, anorexia, nausea and vomiting, diarrhea as well as acute liver failure, hypo/hypermania and psychosis in rare cases. Interactions - avoid of tyramine containing foods which can cause a hypertensive crisis 
Term

Phenylephrine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. α1-receptor selective agonist
  2. Use as a decongestant, treatment of haemorrhoids, pulillary dilation, priaprism treatment and as a vassopressor in hypotension - especially resulting form septic shock
  3. α1-receptor binding causes blood vessel constriction through Gq mediated pathway
  4. High blood pressure (hypertension as contraindication), can cause bradycardia as hypertension causes stimulation of carotid baroreceptors. Can worsen prostatic hyperplasia and cause rebound hyperaemia. Vasoconstriction may causes ischaemic necrosis in tissues
Term

Phenytoin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Anticonvulsant
  2. Use in treatment of tonic-clonic, focal and surgical seizures
  3. Blockade of voltage gated sodium channels and therefore high-frequency, repetitive firing of action potentials. Preferencial binding to inactive sodium channel form causing use-dependent and time-depedent blockade. Primary action within the motor cortex by the stabilisation of threshold against hyperexcitibilty brought on my excessive stimulation or environmental changes reducing post-tetanic potentiation. 
  4. Nausea, stomach pain, loss of coordination, increased hair growth, liver toxicity, low blood presusre and epidermal necrolysis. It is a known teratogen so pregnancy is a contraindication. Possible cause of hypertrichosis, SJS, rush and itching.
Term

Prazosin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Sympatholytic (α1 specific)
  2. Hypertension, urinary hesitancy in prostatic hyperplasia, and for treatment of nightmares in children and PTSD patients (low dose)
  3.  Inverse agonist at α1-adrenoceptors, therefore reducing the vasocontriction of blood vessels through reduction in Gq transduction. This therefore decreases blood pressure, as well as afterload on the heart. However, initially the baroreceptor reflex increases heartrate and contractility as the homeostatic mechanisms attempt to return blood pressure to current set point.
  4. Hypotension associated side effects - dizziness, headache, drowsiness, lethargy, weakness, palpitations. Orthostatic hypotension observed due to lack of control of blood pressure during α1 blockade. Can cause odema, dyspnea, syncope, depression, nervousness and rash. 
Term

Propofol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. General anaesthesia
  2. Part of total intravenous anasthesia, sedation during mechanical ventilation, procedural sedation (e.g. infants in MRIs)
  3. Potentiation of GABAA receptor activity through the slowing of channel closing, as well as a sodium channel blocking agent. Possible interaction with the endocannabinoid system and prominent reduction in the brain information capacity at gamma wave band frequencies
  4. Pain on injection through activation of TRPA1 (pretreatment with lidocaine), hypotension, vasodilation, transient apnea. 
Term

Propranolol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Beta blocker
  2. Hypertension, angina pectoris, tachyarrythmia, MIs, tachcardia associated with anxiety, panic, hyperthyroidism and lithum therapy, portal hypertension, anxiety and asymmetric septal hypertrophy
  3. Non-cardioselective beta blocker that is permeable to the BBB. This reduces the force of contraction within the heart, and thus reduces cardiac workload and arterial blood pressure. Also has sodium channel blocking effects giving local anaesthetic effect. Also acts to marginally increase adrenal release by inhibiting NAd transporter, and therefore acting only on α1 receptors as a weak agonist. 
  4. Sleep disturbances from CNS effects, bronchospasm, peripheral vasocontriction and alteration of glucose and lipid metabolism. Can cause hypotension, bradycardia, heart failure, heart block and fatigue. Contraindications in patients with diabetes, peripheral vascular disease, pheochromocytoma and drugs with bradycardic effects. 
Term

Ramipril

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. ACE inhibitor
  2. Hypertension, congestive heart failure, following heart attch, prophylaxis of stroke, heart attack, CV death, and as treatment for kidney damage with proteinuria
  3. Inhibits action of ACE and therefore prevents the conversion of angiotensin I into angiotension II, while also decreaing the breakdown of bradykinins. Angiotension II acts as a vasopressor, therefore ACE inhibitors release arteriole smooth muscle, decrease total peripheral resistance and blood pressure
  4. Shakiness, faiting, neutropenia, impotence through erectile dysfunction, dry cough (bradykinins), infection, chest pain. Rare severe allergic reactions that may occasionally lead to liver failure
Term

Rifampicin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antibiotic
  2. Treatment of tuberculosis, leprosy, MRSA, N. meningitidis, tick borne pathogens
  3. Inhibition of bacterial DNA-dependent RNA synthesis by inhibiting RNA polymerase. Appears to bind in pocket of RNA polymerase β subunit within the DNA/RNA channel, which physically blocks 5' elongation and therefore prevents synthesis - steric occlusion mechanism
  4. Hepatotoxicity, fever, GI disturbances, immunological reactions, changes colour of body fluids to orange-red. Breathlessness, nausea, vomiting, flu like symptoms and possible allergic reaction
Term

Salbutamol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  • β2 adrenergic agonist
  • Bronchospasm in asthma and COPD. As a tocolytic to relax uterine smooth muscle and as treatment of hyperkalaemia acutely
  • Relaxation of smooth muscle in lung by coupling of βreceptor to Gs protein and thus production of cAMP which decreases calcium ion concentation and activates PKA, inactivating myosin light-chain kinase and activating myosin light chain phosphatase. As well as this, βagonists open large conductance calcium activiated potassium channels and hyperpolarise airway smooth muscle cells leading to bronchodilation
  • Fine tremor, anxiety, headache, muscle cramps, dry mouth and palpitations. Can cause arrythmias, tachycardia and allergic reaction. Possible hypokalaemia in patients with renal failure and those on duiretics/methyl xanthines
Term

Saquinavir

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antiretroviral
  2. Used in the treatment and prevention of HIV/AIDS (usually with ritonavir or lopinavir for increased efficacy)
  3. Protease inhibitor - inhibits HIV protease which is vital for viral replication within the cell and release of mature viral particles from infected cells. Saquinavir binds to protease and prevents polyprotein cleavage and thus viral maturation
  4. Diarrhea, nausea, loose stool and GI discomfort
Term

Sevoflurane

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. General anaesthetic
  2. Inhaled anaesthetic for surgical procedures
  3. Thought to act as a positive allosteric modulator for GABAA as well as acting as a NMDA receptor antagonist, potentiator of glycine receptor currents, and inhibibtion of nAChR and 5-HT3 currents
  4. Raised intracranial pressure and respiratory depression, neurotoxicity (debated), as well as agitation and delerium on waking
Term

Simvastatin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Statin
  2. Treatment of dyslipidemia and prevention of atherosclerosis associated complications. 
  3. Acts by inhibiting HMG-CoA reductase which is the rate limiting step in the endogenous production of cholesterol, and therefore reduces LDL concentrations by up to 50%
  4. Rare side effects. Can include indigestion and eczema, and even rarer joint pain, memory loss and muscle cramp. Cholestatic hepatitis, hepatic cirrhosis, myopathy and rabdomylosis have been reported in chronic administration. 
Term

Spironolactone

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Potassium sparing diuretic
  2. Heart failure, odematous conditions, hypertension, hypokalamia, primary (Conn's)/secondary hyperaldosteronism. Androgen receptor antagonism use for androgenic alopecia, acne and seborrhea.
  3. Displacement of aldosterone from mineralocorticoid receptor in collecting duct of nephron and thus preventing expression of ENaC and ROMK channels in distal nephron as well as directly inactivating aldosterone synthase and thus reducing production. Androgenic activity - blocks andrigen receptor as well as androgen biosynthesis pathway to decrease production of testosterone and DHT
  4. Urinary frequency, dehydration, hyerkalaemia, hyponatraemia, hypotension, ataxia, gynecomastia, tesicular atrophy, reduced fertility and sexual dysfunction.
Term

Steptokinase

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Thrombolytic
  2. IV treatment during STEMI
  3. Complexes with plasminogen to hydrolytically activate unbound plasminogen to produce plasmin. Plasmin then breaks down fibrin to dissolve thrombus
  4. As a bacterial product, can cause immunity and allergic reaction. Contraindications - intracranial haemorrhage, vascular lesion, cranial cancer, history of stroke, aortic dissection, any active bleeding or uncontrolled high blood pressure. 
Term

Sumatriptan

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Serotonin receptor agonist
  2. Resolving or relieving migraines or cluster headaches
  3. Agonist for 5-HT1D/1B receptors which are present on cranial arteries and veins. Activation causes vasocontriction of dilated, inflammed arteries and appears to decrease the activity of the trigeminal nerve, which is implicated in cluster headaches (aborted in 15 minutes of injection in 96% of cases)
  4. Sulfhaemoglobinaemia, coronary artery vasospasm, myocardial ischaemia (transient), MI, ventricular tachycardia and fibriliation. More common side effects - atypical sensations of temperature, chest pain and fatigue.
Term

Suxamethonium 

 (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Paralytic agent
  2. Muscle relaxant in short term anaesthesia or intubation, ECT
  3. Phase 1 block - bind and activation of nAChR causing depolarisation of end plate and calcium release from SR. Receptors remain open when bound to suxamethonium, therefore the Edoes not return to normal potential, preventing the inactivation and subsequent reactivation of VG sodium channels. Phase 2 block involves desensitisation as the constituetively active nAChRs being internalised and the therefore the end-plate desensitised to nervous input. 
  4. Hyperthermia, muscle pain, rhabdomyolysis (with hyperkalaemia), ocular hypertension, constipation and slowing of heart rate. Contraindications include closed head injury, acidosis, cerebral stroke, drowning (?), sepsis, massive trauma, myopathy and tetanus. Absolute contraindication - mutation in buryrylcholinesterase. 
Term

Tamoxifen

 (drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Chemotherapy agent
  2. Early and advanced oestrogen receptor positive (ER+) breast cancer in both pre and post menopausal women. Prophylaxis in women with high risk of breast cancer. Treatment of infertility in anovulatory disorders. Prevention of gynecomastia from elevated oestrogen. 
  3. Conversion by CYP3D6 in liver into active metabolistes 4-OHT and endoxifen. Competition with oestrogen for binding to ER, 4-OHT acting as an antagonist to prevent transcription of oestrogen responsive genes. The ER bound complex recruits co-repressor proteins to modulate gene expression, such as NCoR and SMRT. In presence of high PAX2 expression the complex can suppresion expression of pro-proliferative ERBB2 protein. The complex produces a nuclear complex that decreases DNA synthesis and inhibits oestrogen effects and thus holds cells in the G0/1 phases of the cell cycle (and therefore is cytostatic rather than cytotoxic)
  4. DVT leading to lymphedema, bone loss in premenopausal women, endometrial cancer as acts as ER partial agonist in endometrium, increase in [triglyceride]plasma resulting in CV and metabolic issues such as steatorrhoeic hepatosis, reduced cognition (semantic memory) and possible premature growth plate fusion. 
Term

Temazepam

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Benzodiazepam
  2. Treatment of disabling sleep disorders
  3. Potentiation of GABAA receptor to cause sedative, anti-convulsant and anxiolytic effects
  4. Contraindications - ataxia, hypoventilation, hepatic deficiency, apnea, depression, intoxication, myasthenia gravis, hypersensitivity, special caution in pregnancy and in those with history of substance abuse. Adverse effects include CNS depression, sedation, fatigue, lethargy, memory and learning impairment, as well as less common hyperhyrosis, hypotension, hallucination, faintness, vomiting and palpitations. Tolerance, phsyical dependent and withdrawal may develop (worse than opiate - can lead to mania and schizophrenia in severe cases).
Term

Tetracycline

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antibiotic
  2. Rickettsia, lyme disease, Q fever, psittacosis, lymphogranuloma and nasal carriage of meningococci. Also used to treat acne, cholera, brucellosis, plague and syphilis. 
  3. Inhibiton of protein synthesis by blocking attachment of charged tRNA to A site on ribosome. This prevents introduction of amino acids into the growing peptide. Although tetracycline acts on both bacterial and mammalian cells, the bacteria actively pump tetracycline across the cell wall, and therefore it is far more effective in inhibiting bacterial translation. 
  4. Side effects often problematic - teeth discolouration, inactivation by calcium, aluminium, iron and zinc ions, causing photosensitivity, drug induced LE and hepatitis, tinnitus and can alter fetal bone growth.
Term

Tramadol

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Opioid analgesic
  2. Treatment of mild to severe pain,
  3. μ-opioid receptor agonist, serotonin reuptake inhibitor and releasing agent, NAd reuptake inhibitor, NMDA receptor antagonist, 5-HT2C receptor antagonist, nAChR antagonist, TRPV1 agonist, and M1/3 antagonist. Naloxone only partially reverses the analgesic effect, so likely to be caused, in part, by other receptor interactions. Antagonist of 5-HT2C is thought to give anti-depressant and OCD symptom effects, while also lowering seizure threshold. 
  4. Nausea, dizziness, dry mouth, indigestion, vertigo, vomiting and headache. Respitory depression less common compared to other opioids. Interaction with most anti-depressant, anxiolytic and anti-psychotic drugs. Causes opioid physical dependence and withdrawal
Term

Trastuzumab

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Chemotherapy agent
  2. Treatment of metastatic breast cancer
  3. HER2 gene is amplified in 20-30% of early stage brest cancers. Trastuzumab activates p27 by inhibiting Pl3K/Akt, Mirk and hKlS pathways, which cause the overexpression of HER in the cell membrane. HER2 pathway normally promotes growth and division, but in overexpression this is accelerated and hence can be exploited for tumour formation. EGF pathway is activated with the binding of EGF to HER receptors, whih initates MAP kinase, Pl3 kinase/Akt and NF-κB pathways. Transtuzumab binds to HER2/neu receptor to arrest mitosis, as well as downregulating Akt activation and suppressing angiogenesis by induction of antiangiogenic factors. p27 induction is thought to play a role in these mechanisms.
  4. Flu like symptoms, nausea, vomiting and diarrhea. Serious symptoms can include cardiac dysfunction, as NRG-1 (essential for cardiomyocyte cell survival) is downregulated. Therefore patients pre-existing heart problems are contraindicated. 
Term

Trimethoprim

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antibiotic
  2. UTIs, middle ear infections, diarrhea, P. jiroveci pneumonia treatment, treatment of any susceptible aerobic bacterial species
  3. Binds to dihydrofolate reductase to inhibit production of THF. THF is essential in the synthesis of thymidine, and therefore inhibition of bacterial DNA synthesis. Affinity for bacterial dihydrofolate reductase is several thousand times greater than affinity for human version of enzyme. 
  4. Nausea, vomiting, diarrhea, rash, photosensitivity, itchiness, thrombocytopenia through lowering folic acid levels, action on eNaC channels (similar to amiloride) so has diuretic and hyperkalaemic effects.
Term

Valproate

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Anti-convulsant
  2. Treatment of epilepsy (tonic-clonic, absence, myoclonic, and second line for partial and infantile seizures). Treatment of manic symptoms of BD and prevention of migraines. 
  3. Increasing CNS levels of GABA, possibly through inhibition of GABA degenerative enzymes such as GABA transaminase or inhibiting GABA reuptake mechanisms. Also may prevent hyperexcitability through action of Kv7.2 channels and AKAP5, and prevents seizure induced reduction of PIP3.  Valproate has histone deacetylase-inhibiting effects and therefore maintains active chromatin to produce neuroprotective effects - possibly mediated by VEGF, BDNF and GDNF. 
  4. Nausea, drowziness, dizziness, vomiting and weakness are common. Bleeding, thrombocytopenia, encephalopathy, suicidal behaviour and hypothemia are less common but more serious. Cause of hepatotoxicity, pancreatitis and fetal abnormalities. Contraindications include pregnancy, liver dysfunction, pancreatitis, porphyria or mitochondrial disease
Term

Vecuronium

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Muscle relaxant
  2. Surgery, mechanical ventilation, intubation (suxamethonium preferred)
  3. Competitive antagonist for nAChR at motor endplate, preventing the depolarisation of the endplate and therefore inhibiting the opening of VG sodium channels followed by calcium channels and muscle contraction. 
  4. Low blood pressure, rare allergic reaction.
Term

Venlafaxine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. SNRI
  2. Treatment of depression, general anxiety disorder, social phobia, panic disorder. Off label perscription for diabetic neuropathy and migraine prophylaxis. Possibly use in cataplexy, narcolepsy, ADHD and PTSD
  3. Appears to prevent reuptake of serotonin and NAd, as well as dopamine to some extent. Indirect effects on opioid receptors and α2 receptors appear to increase pain threshold experimentally. 
  4. Increased suicide risk, SSRI discontinuation syndrome (dysphoria, headache, nausea, sleep disturbance), serotonin syndrome (autonomic instability, neuromuscular abberations, GI symptoms). Contraindications - glaucoma and pregnancy
Term

Vincristine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Chemotherapy agent
  2. Non-Hodgekin's lymphoma, Hodgekin's lymphoma, nephroblastoma and in acute lymphoblastic/childhood leukaemia. 
  3. Binds to tubulin protein, therefore preventing the cell from seperating chromosomes during metaphase of mitosis causing cell apoptosis. 
  4. Peripheral neuropathy, hyponatraemia, constipation and hair loss. 
Term

Warfarin

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Anticoagulant
  2. DVT, pulmonary embolism, prevention of stroke in: AF, valvular heart disease and artificial heart valves. Sometimes used following STEMI and in orthopedic surgery.
  3. Inhibition of vit K dependent synthesis of clotting factors II, VII, IX and X as well as regulatory factors protein C, S and Z. Specifically, warfarin inhibits epoxide reductase, diminishing the availability of vit K in tissues, preventing carboxylation of coagulation factors and preventing them from binding to endothelial surfaces of blood vessels. Due to effects on regulatory proteins C, S and Z, warfarin temporarily increases clot formation.
  4. Common side effect - bleeding. Can also cause warfarin necrosis through protein C inhibition mediated clotting in vessels leading to skin and limb necrosis. Link between warfarin use and osteoporosis. Interaction with many commonly used drugs, while antibiotics may inhibit warfarin breakdown and thyroid activity influences dosing requirements. 
Term

Zidovudine

(drug class, medical uses, mechanism of action, notable side effects/contraindications)

Definition
  1. Antiretroviral
  2. Treatment and prophylaxis of HIV/AIDS
  3. Thymidine analogue and therefore selectively inhibits reverse transcriptase preventing the production of double stranded DNA from RNA and integration into host genome. 
  4. Nausea, vomiting, acid reflux, headache, light sleeping and loss of appetite. Higher dose therapy side effects can include anaemia, neutropenia, hepatotoxicity, cardiomyopathy and myopathy thought to be caused by depletion of mDNA, sensitivity of γ-DNA polymerase in mitochondria to zidovudine, depletion of thymidine triphosphate, oxidative stress, reduction in intracellular L-carnitine or apoptosis. Viral resistance can develop from mutations in reverse transcriptase and thus given as combination therapy.
Supporting users have an ad free experience!