Term
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Definition
Used for: allergy, cardiac arrest
Non-selective adrenergic agonist that acts on both alpha and beta adrenoceptors
Alpha1 = vasoconstriction
Beta1 = increase rate and force of cardiac contractions
Beta2 = bronchodilation, stabilisation of mast cells |
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Term
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Definition
General Anaesthetic
Mechanism not fully understood
Thought that the gas interacts with the plasma membranes of nerve cells in the brain and thus affects the communication among such cells at their synapses, resulting in anaesthesia |
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Term
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Definition
General Anaesthetic
Unknown, thought to interact with GABAa receptor to mimic GABA (inhibitory neurotransmitter) or to potentiate its actions |
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Term
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Definition
General Anaesthetic
A non-depolarizing competitive antagonist acting at the nicotinic ACh receptor (nAChR) on skeletal muscle to cause muscle relaxation |
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Term
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Definition
General Anaesthetic
Depolarising muscle relaxant
Acts by stimulating the neuromuscular endplate (nicotinic agonist) and blocking repolarisation thus preventing normal neuromuscular transmission
Different to non-depolarising (which are competitive antagonists at nicotinic receptor)
Provides the most rapid, reliable onset |
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Term
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Definition
General Anaesthetic
In ionised form, binds to the inside of voltage-gated Na+ channels inhibiting the influx of Na+and preventing further depolarisation from occurring --> reversible local anaesthetic
Shorter half life than lignocaine |
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Term
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Definition
General Anaesthetic
In ionised form, binds to the inside of voltage-gated Na+ channels inhibiting the influx of Na+and preventing further depolarisation from occurring --> reversible local anaesthetic
Longer half life than lignocaine |
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Term
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Definition
General Anaesthetic - amide anaesthetic
In ionised form, binds to the inside of voltage-gated Na+ channels inhibiting the influx of Na+and preventing further depolarisation from occurring --> reversible local anaesthetic |
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Term
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Definition
Antidote
Rapidly enters cells where it is hydrolysed to cysteine resulting in the restoration of glutathione levels, which are needed to detoxify hepatocytes after paracetamol use |
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Term
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Definition
Antidote
Ingested toxic substances present in the gastrointestinal tract bind to the surface of the activated charcoal and as a result are not absorbed. |
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Term
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Definition
Antidote
Works by binding to the venom components and neutralising their effects. The antivenom-venom complex is then excreted |
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Term
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Definition
Antidote
Returns myocyte excitability back to normal, after mild hyperkalaemia leads to an increase RMP
Also used in treatment of calcium channel blocker poisoning where increasing extracellular [Ca2+] can antagonise effects of these drugs |
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Term
| Digoxin-specific antibody |
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Definition
Antidote
Binds to digoxin with high affinity removing it from the site of action |
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Term
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Definition
Diabetes, Antidote
Increases blood glucose levels by stimulating glycogenolysis and gluconeogenesis, thus opposing the effects of insulin
Can be used to treat overdose of beta-clockers of calcium channel blockers as it increases the rate and force of cardiac contractions via an increase in cAMP (the second messenger for β-adrenoceptors) |
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Term
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Definition
Antidote
A competitive mu-opioid receptor antagonist that also has some antagonist effect at delta- and kappa-opioid receptors
Used to treat opioid overdose |
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Term
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Definition
Angina, Hypertension
Beta-blocker
Is cardioselective i.e. it blocks only the beta1 adrenoceptors found predominantly in the heart
Most common used beta blocker, relatively long half life
Reduces symptoms of effort angina, reduce HR and myocardial contractility, decrease O2 requirements |
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Term
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Definition
Angina
Nitrate
Nitrates are prodrugs which are converted inside cells to nitric oxide
Causes vasodilatation
Unlike beta-blockers and calcium antagonists, can be used safely in people with cardiac failure |
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Term
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Definition
Arrhythmia
P1 receptor agonist
Hyperpolarises cardiac conducting tissue and slows pacemaker activity via A1receptors at the atrioventricular node
Most commonly used to terminate (re-entrant) supraventricular tachycardia (SVT) |
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Term
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Definition
Arrhythmia
Predominantly K+ channel blocker which prolongs duration of action potential and increases effective refractory period
Also has anti-adrenergic and calcium channel blocker effects |
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Term
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Definition
Arrhythmia
inhibits Na+/K+ ATPase. This causes an increase in intracellular sodium and then calcium, through ion exchange. Has some direct anti-adrenergic and vagal effects
Most commonly used as AV block for atrial fibrillation
Good in clinical heart failure as positive inotropic effects |
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Term
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Definition
Arrhythmia
Calcium channel blocker
Is a phenylalkylamine calcium channel blocker which blocks L channels and inhibits the inward passage of calcium ions through these channels |
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Term
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Definition
Heart failure
Loop diuretic
Inhibits the absorption of sodium chloride from the ascending limb of the Loop of Henle by inhibiting the Na+/K+/2Cl- carrier |
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Term
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Definition
Heart failure, Hypertension
ACE inhibitor
Inhibit the conversion of angiotensin I to angiotensin II |
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Term
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Definition
Heart failure
K+ sparing diuretic
A synthetic steroid which competes with aldosterone for mineralocorticoid receptors and inhibits aldosterone's Na+-retaining K+-excreting action at the distal nephron (predominantly in the collecting tubule) |
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Term
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Definition
Hyperlipidaemia
Statin
Is an inhibitor of the enzyme HMG CoA
HMG-CoA reductase inhibitors inhibit the enzyme responsible for catalysing theproduction of mevalonate which is an early rate-limiting step in the biosynthesis of cholesterol. |
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Term
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Definition
Hypertension
Calcium channel blocker
Blocks L channels and inhibits the inward passage of calcium ions through these channels |
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Term
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Definition
Hypertension
Thiazide diuretic
Inhibits the action of the Na+/Cl- cotransport system in the upper part of the ascending limb of the Loop of Henle and in the distal convoluted tubule |
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Term
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Definition
Hypertension
Sartan
An angiotensin II subtype 1 (AT1) receptor antagonist and inhibits angiotensin II from binding to its receptor, thereby preventing it from exerting most of its effects |
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Term
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Definition
Thromboembolic Disease
COX inhibitor
Irreversibly inhibits platelet cyclo-oxygenase, thereby reducing the formation of TXA2 and abolishing the ability of platelets to aggregate
Dose dependent kinetics |
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Term
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Definition
Thromboembolic Disease
Inhibits ADP-induced activation of platelets by inhibiting binding of ADP to the platelet receptor and prolonging bleeding time
Is a pro-drug |
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Term
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Definition
Thromboembolic Disease
Low molecule weight heparin (LMWH)
Chain lengths with LMW heparins are mostly insufficient to allow factor IIa inactivation and therefore the activity of LMW heparins is predominantly via antithrombin III accelerating inactivation of clotting factor Xa |
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Term
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Definition
Thromboembolic Disease
Heparin chains contain binding sites to antithrombin III. When antithrombin III binds to these sites, its activity increases allowing it to inactivate certain clotting factors and as a result the process of coagulation will slow down
Not absorbed orally |
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Term
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Definition
Thromboembolic Disease
Thrombolytic
A protein produced by several strains of streptococci
It forms a complex with plasminogen leading to the conversion of plasminogen to plasmin
Plasmin digests fibrin |
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Term
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Definition
Thromboembolic Disease
Coumarin (vit K antagonist)
Inhibits the hepatic production of clotting factors 2, 7, 9, and 10
The synthesis of these proteins involves the conversion of reduced vitamin K to its epoxide
This drug blocks the conversion of the epoxide back to vitamin K
Therapeutic delay 2-7 days |
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Term
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Definition
Bone disorders
Bisphosphate
Bisphosphonates are adsorbed onto hydroxyapatite crystals (the crystalline form of calcium and phosphate) in bone, slowing both their rate of growth and dissolution, and therefore reducing the rate of bone turnover
They reduce bone resorption by osteoclasts, hinder recruitment of osteoclasts, and stimulate osteoblasts to produce an inhibitor of osteoclast formation |
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Term
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Definition
Bone disorders
Active form of vit D
Maintain plasma Ca2+ levels by stimulating Ca2+ and phosphate uptake in the gastrointestinal tract, mobilising Ca2+ from bone and decreasing Ca2+ excretion at the kidney
Vitamin D supplements endogenous stores of Ca2+ and consequently increases calcium uptake and retention and supports the mineralisation of the skeleton |
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Term
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Definition
Diabetes
Sulphonylurea
Block KATP channels on pancreatic beta cells causing depolarisation and an influx of Ca2+resulting in the release of insulin
Used when diet, exercise and usually metformin have not worked. Can use first instead of metformin in non-obese type 2 |
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Term
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Definition
Diabetes
The binding of insulin to the insulin receptor, a tyrosine kinase receptor, results in a variety of actions including lowering blood glucose levels
Given subcutaneously 30 mins before food, duration 4-6 hrs (can cause hypoglycaemia after meal), made of recombinant DNA |
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Term
| Insulin - Intermediate and long acting |
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Definition
Diabetes
The binding of insulin to the insulin receptor, a tyrosine kinase receptor, results in a variety of actions including lowering blood glucose levels
Addition of zinc or protamine delay absorption
Usually given with short-acting twice daily, or at night time for basal level |
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Term
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Definition
Diabetes
Increases the effectiveness of insulin in promoting glucose uptake into cells. It also decreases hepatic glucose production |
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Term
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Definition
Diabetes
Glitazone
Binding of glitazones with PPAR-gamma (nuclear receptor found in adipose tissue) activates adipocyte differentiation, increases lipogenesis and enhances the uptake of fatty acids and glucose
Glitazones increase a patient's sensitivity to insulin (unknown why) |
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Term
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Definition
Hyperthyroidism
Interferes with the organification of iodine (not the uptake of iodine), by inhibiting iodine binding to tyrosine. Additionally it has an inhibitory effect on thyroid peroxidase, which acts as a catalyst in the production of thyroxine
Takes 4-6 weeks to be effective |
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Term
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Definition
Hypothyroidism
Mimics the effects of normal thyroid hormone (T4) including suppression of TSH |
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Term
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Definition
Constipation
Osmotic laxative
Broken down in the colon by bacteria to predominantly lactic acid and small amounts of acetic and formic acids which acidifies the colon contents. This in turn draws water into the colon resulting in an increase in stool water content and softer stools |
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Term
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Definition
Constipation
Mechanism unknown
Suggested that anthraquinone glycosides found in the leaves are hydrolysed to active anthraquinone which then acts in the colon to stimulate the myenteric plexus, increasing peristalsis and defecation |
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Term
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Definition
Diarrhoea
Opioid agonist
Activation of predominantly mu-opioid receptors located in the myenteric plexus and intestines results in increased smooth muscle tone, decreased peristalsis and decreased secretions |
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Term
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Definition
GORD/PUD
Proton pump inhibitor
After systemic absorption, it diffuses into the parietal cells and in this acidic environment they are converted from a prodrug into an active drug that reduces gastric acid secretion by irreversibly inhibiting the H+/K+ ATPase |
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Term
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Definition
GORD/PUD
Competitive H2 receptor antagonist
Blocks the actions of histamine at H2 receptors and as a result inhibits histamine-induced gastric acid secretion |
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Term
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Definition
Nausea and vomiting
D2 dopamine antagonist
The antiemetic effects are predominantly due to an inhibition of D2 receptors (which stimulate vomiting centre) in the CTZ, however increased gastric emptying, as a result of inhibition of D2 receptors in the gut, also contributes to this effect
Also weak 5HT3 antagonist |
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Term
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Definition
Nausea and vomiting
5HT antagonist
Blocks 5HT3 receptors located on vagal afferents and in the CTZ |
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Term
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Definition
Obesity
Binds to lipases irreversibly inhibiting the enzymes from breaking down triglycerides
Indicate for adults with BMI >30 or >27 if other risk factors present |
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Term
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Definition
Antihelmintic
Benzimidazole
Binds to free β-tubulin preventing polymerisation causing deterioration of the microtubules to occur.
Also disrupts glucose uptake and leads to a depletion of energy stores and the subsequent immobilisation and death of the organism |
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Term
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Definition
Antihelmintic
Broad-spectrum anti-parasitic drug
Mechanism unknown
Thought to open glutamate-gated chloride channels which causes an influx of Cl- ions resulting in hyperpolarisation of the cell leading to neuromuscular paralysis and death of the parasite |
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Term
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Definition
Antibacterial
Broad-spectrum penicillin
Inhibits the synthesis of bacterial cell walls by binding to the transpeptidase enzyme preventing the final cross-linking phase of peptidoglycan synthesis resulting in a weak cell wall and subsequent osmotic lysis of the dividing bacterium |
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Term
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Definition
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Term
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Definition
Antibacterial drug
Bacteriostatic broad-spectrum antibiotic
Binds to the 50S subunit of the bacterial ribosome and inhibits protein synthesis
Works against Gram-+ve and Gram--ve aerobic and anaerobic organisms |
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Term
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Definition
Antibacterial
Quinolone antibiotic
Inhibits DNA synthesis in bacteria by inhibiting the activity of two enzymes, topoisomerase II (DNA gyrase) and topoisomerase IV |
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Term
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Definition
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Term
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Definition
Antibacterial
Macrolide antibiotic
Binds reversibly to the 50S subunit of the bacterial ribosome, and interfere with bacterial protein synthesis
Broad spectrum
Can be bacteriostatic or bactericidal, depending on conc in blood or tissue |
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Term
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Definition
Antibacterial
Aminoglycoside
Inhibit protein synthesis by binding irreversibly to the 30S subunit of the bacterial ribosome causing the ribosome to misread the mRNA
Aminoglycosides have a broad Gram-negative spectrum and are active against Staphylococcus aureus
Not very effective against anaerobes as actions if O2 dependent |
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Term
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Definition
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Term
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Definition
Antibacterial
Nitroimidazole
Is taken up by anaerobic organisms and is reduced by microbial nitroreductase to an unstable intermediate product which interacts with DNA to inhibit nucleic acid synthesis and prevent further replication
Active against Gram+ and Gram- |
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Term
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Definition
Antibacterial
Binds to the β subunit of bacterial DNA-dependent RNA polymerase resulting in suppression of RNA synthesis in susceptible bacteria
Effective against Gram+ bacteria |
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Term
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Definition
Antibacterial
Glycopeptide antibiotic
Inhibits peptidoglycan synthesis, causing a weakening of the cell wall resulting in osmotic lysis of the bacterial cell |
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Term
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Definition
Antifungal
Polyene antifungal drug
Binds to ergosterol in the fungal cell membrane and forms amphotericin-B pores which alter cell permeability resulting in cell death |
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Term
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Definition
Antifungal
Azole antifungal
Inhibits the fungus-specific cytochrome P450 enzyme 14α-sterol demethylase, which is an enzyme that converts lanosterol into ergosterol |
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Term
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Definition
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Term
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Definition
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Term
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Definition
Antiviral
Inhibits viral DNA synthesis by inhibiting viral DNA polymerase and also by incorporating into the viral DNA resulting in chain termination
It is a nucleoside analogue which selectively inhibits the replication of herpes simplex virus (types 1 and 2) and varicella zoster virus |
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Term
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Definition
Antiviral
An oral prodrug used in the treatment of influenza A and B and in the prophylaxis of influenza
Following hepatic metabolism, active oseltamivir carboxylate binds to the viral neuraminidase and blocks its ability to cleave sialic acid thereby preventing the virus from being released. |
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Term
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Definition
Antiviral
Nucleoside reverse transcriptase inhibitor
Acts as a chain terminator as it lacks the 3'-OH group required for DNA chain elongation |
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Term
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Definition
Antineoplastic
A non-selective aromatase inhibitor and hence causes a decrease in circulating levels of oestrogen and therefore reduced growth of oestrogen-dependent breast cancer cells |
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Term
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Definition
Antineoplastic
a nitrogen mustard alkylating agent that has both cytotoxic and immunosuppressive actions
Is a prodrug |
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Term
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Definition
Antineoplastic
Three different mechanisms
1- It intercalates with DNA causing structural changes which can inhibit transcription and replication
2- It binds to DNA and topoisomerase II forming a complex which prevents religation of broken DNA strands
3- It generates reactive oxygen species that can damage DNA |
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Term
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Definition
Antineoplastic
Is converted intracellularly to several active metabolites: FdUMP, FUTP, and FdUTP, all have cytotoxic actions |
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Term
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Definition
Antineoplastic, DMARD, Immunomodulator
Its cytotoxic actions are a result of it acting as a competitive inhibitor of dihydrofolate reductase (DHFR), an enzyme involved in converting folic acid to tetrahydrofolate
Tetrahydrofolate is essential, and if depleted, results in the inhibition of DNA and RNA synthesis
The mechanism(s) of methotrexate's anti-inflammatory and immunosuppressive effects are still unclear |
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Term
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Definition
Antineoplastic
Selective oestrogen receptor modulator (SERM)
Depending on the target tissue has either antioestrogenic or oestrogenic effects
In breast tissue the action of tamoxifen is antioestrogenic, hence its use in ER-positive breast cancer where it acts as an antagonist at ER receptors and suppresses the growth of oestrogen-dependent breast cancer cells |
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Term
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Definition
Antineoplastic
A monoclonal antibody that inhibits proliferation and survival of HER2-dependent tumours by binding to the extracellular domain of the HER2 receptor and preventing activation of the intracellular tyrosine kinase |
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Term
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Definition
Immunomodulator
Inhibits signalling transduction pathways required for T cell activation |
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Term
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Definition
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Term
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Definition
Immunomodulator
Glucocorticoid
Upon binding of glucocorticoid agonists, the GR (glucocorticoid receptor) disassociates and is translocated into the nucleus where it then brings about its effects either by binding to glucocorticoid response element (GRE) to regulate gene transcription or interacting with other transcription factors |
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Term
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Definition
Immunomodulator
This prevents the T cells from moving from the G1 to S phase suppressing T cell proliferation |
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Term
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Definition
DMARD
An antibody that blocks the effects of tumor necrosis factor alpha (TNF alpha) and is administered by I.V.
TNF alpha is a pro-inflammatory cytokine that has a major role in promoting inflammation |
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Term
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Definition
DMARD
Mechanism unknown
Reduces cytokine production and decreases the inflammatory response
Combo of antibiotic and aspirin derivative |
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Term
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Definition
Gout
Inhibits xanthine oxidase, an enzyme involved in the production of uric acid from hypoxanthine and xanthine (purine degradation products).
Used in patients with multiple recurrent gout attacks and kidney disease caused by uric acid or urate deposition |
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Term
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Definition
Gout
Disrupts the cytoskeleton assembly resulting in the inhibition of several cellular functions including cell division, secretion of mediators and intracellular vesicle transport, with the greatest effect seen in cells that have a high turnover (e.g. neutrophils). |
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Term
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Definition
NSAID
Inhibit COX thereby inhibiting prostaglandin synthesis - COX-1 and COX-2
COX-1 = adverse GI effects and antiplatelet effects
COX-2 = analgesic and anti-inflammatory |
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Term
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Definition
NSAID
More selective for COX-2 so has analgesic and anti-inflammatory properties with less adverse effects on the gastrointestinal tract
However there still appears to be a risk of renal side effects |
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Term
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Definition
Asthma
Long Acting Beta-2 agonist
binds to bronchial β2-adrenoreceptors causing smooth muscle relaxation
Duration 8-12 hrs |
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Term
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Definition
Asthma
Glucocorticoid
Binds to the intracellular glucocorticoid receptor (GR) resulting in a reduction of the inflammatory response |
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Term
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Definition
Asthma
Short acting beta-2 agonist
Binds to bronchial β2-adrenoreceptors causing smooth muscle relaxation
Duration 3-6 hrs |
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Term
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Definition
Infertility
Used as first-line ovulation induction in women with anovoluntary infertility or PCOS
It acts by inhibiting oestrogen feedback at the level of the hypothalamus and by enhancing gonadotrophin stimulation of follicular development. Administration results in increased luteinizing hormone (LH) and follicle stimulating hormone (FSH) |
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Term
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Definition
Labour
The two main actions are contraction of uterine muscle and milk release during lactation which are mediated via activation of this drug’s receptors |
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Term
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Definition
Urogenital
It is drug is a 5α-reductase inhibitor which inhibits the conversion of testosterone to DHT therefore decreasing DHT levels and consequently reducing the size of the prostate and improving urinary symptoms
Early development and normal growth of the prostate relies on the androgen dihydrotestosterone (DHT) |
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Term
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Definition
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Term
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Definition
Urogenital
It is an α1adrenoceptor antagonist that shows selectivity for the α1A subtype and α1D subtype over the α1B subtype. Blockade of adrenoceptors causes relaxation of smooth muscle in the prostate and bladder leading to improved urine flow and reduced symptoms of BPH. |
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Term
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Definition
Antipsychotic
Phenothiazine
As with all antipsychotics the exact mechanism of action is still unclear however is predominantly attributed to the blocking of dopamine D2 receptors. In addition chlorpromazine also blocks dopamine D1 receptors, alpha1-adrenoceptors, muscarinic ACh receptors, histamine H1 receptors and 5-HT receptors.
Has lower potency at D2 receptors than haloperidol but has ore anticholinergic side effects |
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Term
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Definition
Antipsychotic
A butophenone
As with all antipsychotics the exact mechanism of action is still unclear however is predominantly attributed to the blocking of dopamine D2receptors. In addition haloperidol also blocks 5-HT receptors and α1-adrenoceptors
Fewer anticholinergic effects than chlorpromazine and doesnt cause sedation, but more extrapyramidal effects |
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Term
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Definition
Anxiolytics & Hypnotics
A benzodiazepine
Binds to the GABAA receptor at a site (called the benzodiazepine binding site) which is distinct from the GABA binding site to potentiate the response of GABA (i.e. increase Cl- influx).
Note that GABA must be bound for benzodiazepines to have an effect, benzodiazepines alone cannot open the Cl- ion channel. |
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Term
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Definition
Anxiolytics & Hypnotics
A non-benzodiazepine hypnotic
Binds to the benzodiazepine site on GABAA receptors to potentiate the response of the inhibitory neurotransmitter GABA (i.e. increase Cl- influx) |
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Term
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Definition
Depression/Bipolar disorder
A tricyclic antidepressant (TCA)
The antidepressant effect of amitriptyline is due to inhibiting serotonin and noradrenaline reuptake and increasing the availability of these neurotransmitters at brain synapses
At low concentrations it also blocks histamine receptors leading to sedation and its antipruritic effect
As doses are increased it also blocks muscarinic receptors and alpha-adrenoreceptors |
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Term
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Definition
Depression/Bipolar disorder
A selective serotonin reuptake inhibitor (SSRI)
SSRIs have a selective effect on the serotonin reuptake pump causing an initial increase in serotonin at the cell body and dendrites and inhibition of the rate of firing of serotonin neurons and release of serotonin
Longer-term exposure causes down regulation of serotonin autoreceptors and disinhibition of serotonin release at axon terminals
With MAOIs or TCAs = increases the risk of serotonin toxicity and serotonergic effects - potentially fatal |
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Term
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Definition
Depression/Bipolar disorder
Inhibits the calcium-dependent release of noraderenaline and dopamine, enhances serotonin release and inhibits the hydrolysis of inositol phosphate in the brain
Narrow therapeutic window - can cause serious disturbances to thyroid, renal, or CNS systems |
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Term
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Definition
Depression/Bipolar disorder
Is a non-selective (inhibits MAO-A and MAO-B), irreversible MAO inhibitor (MAOI). It is thought that phenelzine's antidepressant effects are due to an initial increase in levels of the CNS transmitters serotonin, noradrenaline and dopamine followed by a down-regulation of their respective receptors
MAO is an enzyme that metabolises catecholamines and is found in the CNS and some peripheral organs. There are two type MAO-A and MAO-B |
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Term
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Definition
Drug Dependence
It is a synthetic opioid analgesic with similar mechanism of action to that of morphine (mu opioid receptor agonist).
It has a long elimination half-life of up to 72 hours |
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Term
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Definition
Drug Dependence
Mimics the affects of acetylcholine at nicotinic acetylcholine receptors (nAChRs) in the CNS and autonomic ganglia |
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Term
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Definition
Anti-epileptic
Is a tricyclic compound
Like phenytoin, it blocks sustained high-frequency repetitive firing of action potentials due to blockade of sodium channels
Rate of absorption varies widely between patients |
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Term
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Definition
Anti-epileptic
Is a barbiturate
The mechanism of action is still unclear.
At low doses it binds to the GABAA receptor, at a site independent to that of the benzodiazepines, and potentiates the effects of the inhibitory neurotransmitter GABA by increasing the duration of Cl- influx.
At higher doses it can act directly on the GABAA receptor as a weak agonist.
It also decreases the effects of the excitatory neurotransmitter glutamate by inhibiting the AMPA subtype of glutamate receptors. These effects both contribute to the anticonvulsant activity of this drug by raising the seizure threshold |
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Term
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Definition
Anti-epileptic
It blocks sustained high-frequency repetitive firing of action potentials by maintaining sodium channels in the inactivated state
Absorption is highly dependent on the formulation of the dosage form |
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Term
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Definition
Anti-epileptic, used to treat epilepsy, migraines, neuropathic pain
The mechanism of action of this drug is unclear and it is thought that its action against partial seizures is due to it blocking sustained high-frequency repetitive firing of neurons by blocking sodium channels.
It also decreases GABA metabolism (i.e. increases GABA levels) which may also contribute to its mechanism of action
It is well absorbed with a bioavailability greater than 80%.
It has a small volume of distribution at 0.15L per kg |
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Term
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Definition
Parkinson’s Disease
It is an anticholinergic drug which is a competitive antagonist of muscarinic ACh receptors. Inhibition of muscarinic ACh receptors helps to correct the imbalance between low levels of dopamine and high levels of ACh
Normal voluntary body movement relies on a balance between dopaminergic and cholinergic neurotransmission in the corpus striatum |
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Term
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Definition
Parkinson’s Disease
Is an ergot derivative
Itis a dopamine agonist which increases dopaminergic neurotransmission by directly activating post-synaptic dopamine receptors
Parkinson's disease is associated with low levels of dopamine due to a loss of dopaminergic nerves in the substantia nigra
Benefits over levodopa = do not require enzymatic conversion to active metabolite, have no potentially toxic metabolites, do not compete with other substances for active transport in the blood and across the blood brain barrier |
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Term
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Definition
Parkinson’s Disease
Is a metabolic precursor of dopamine, which is actively transported across the blood brain barrier, unlike dopamine itself.
It is is then decarboxylated by dopa decarboxylase to dopamine within surviving nigrostriatal neurons to correct the consequences of local dopamine depletion
Is absorbed by an active transport mechanism in the small intestine |
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Term
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Definition
Parkinson’s Disease
Is an irreversible inhibitor of MAO-B. By inhibiting MAO-B the breakdown of dopamine is slowed and its actions are prolonged |
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