Pharmocology Flashcards
Proton Pump Inhibitors:
What do the names of the drugs end in? What is a prodrug? What is their protective coating made from? What cells are they taken up by? What do they form in the blood? Why do they last a few days?
Name: ‘zole’ Prodrug: Enters inactive Protective coating: H2CO3- to alter pH Uptake: Parietal cells Form: Suldenamides in the blood Long lasting: Irreversibly bind
Histamine (H2) Antagonists:
What is the normal action of Histamine?
What do H2 antagonists do?
What do the names of the drugs end in?
Action: Binds to H2 receptor –> G protein –> adenylate cyclase –> cAMP –> Protein kinase A –> protein phosphorylation and activation –> increases acid
Antagonists block this
Name: ‘tidine’
NSAIDS’s:
What is the normal action of the COX1 enzyme?
What is the normal action of the COX2 enzyme?
What do NSAID’s do?
COX1: Prostaglandin increase mucus and decrease acid in the stomach
COX 2: Cause inflammation due to illness
Drugs: Stop the inflammation but also decrease mucus and increase acid in the stomach
Misoprostal:
What molecule is it a similar shape to?
What does it do in the stomach?
Similar shape to prostaglandin
Maintains mucus
Muscarinic antagonists:
What do they treat?
What do the names of the drugs end in?
Side effects?
Treat: Motion sickness
Name: ‘cine’
Side effects: Blurred vision, relaxed gut and dry mouth
Histamine (H1) Antagonists:
What do they treat?
What do the names of the drugs end in?
Side effects?
Treat: Motion and morning sickness
Name: ‘zine’
Side effects: Drowsiness and dry mouth
What drug which was used for morning sickness was banned and why?
Thalidomine
Developmental problems in the limbs
5HT3 antagonists:
How do they work?
How can you increase their effectiveness
Target 5HT stimulation
Other drugs for sickness:
Metaclopramide: How it works and side effects.
Phenothiazides: What do the drugs end in and side effects
Doperidone: What does it act on and what can it not cross?
Metaclopramide:
Acts on the chemoreceptor trigger zone and increases digestive motility.
Side effects: movement+menstruation disorders, fatigue, increased prolactin
Phenothazides:
‘zine’ and neurological effects
Doperidone:
Acts on chemoreceptor trigger zone and the gut
Cannot cross the blood brain barrier
2 interventions for autoimmune disease
What do these drugs do?
Rituximab
Atabercept
Ipilumumab
Cytokine therapies block the problematic antibody (e.g. anti-TNF/anti-IL1)
Steroids to stop clonal expansion by blocking receptors and signal recognition
Rituximab: Anti B cell antibodies
Atabercept: Inhibits T cell response by blocking positive signals
Ipilumumab: Stimulates antibody causing positive signal and decreased T cell activity
Name 2 anti-platelet drugs
Aspirin and Clopidogrel
What 2 things does Aspirin do in the vasculature?
3 uses and one problem
Inhibits COX 1 which is used to activate thromboxane A2
Inhibits COX2 in vasculature endothelial cells causing decreased inflammation
Uses: Angina, heart attacks, stroke (can also cause stroke)
What type of drug is Clopidogrel?
What does it do?
How is it metabolised?
Side effect?
Clopidogrel: An ADP receptor antagonis Inhibits ADP (a platelet agonist released from dense granules) Metabolised by P450 enzymes Side effects: Bleeding
What do anti-coagulants do?
What are the 2 types?
Name 2 anti-coagulant drugs
Decrease the formation of fibrin by inhibiting the synthesis/activity of clotting factors
Direct thrombin inhibitors / direct factor 10 inhibitors
Heparin and Warfarin
What are the two types of Heparin and how are they made?
What are the differences between them?
Unfractionated Heparin is a natural polysaccharide which can be fractionated to LMW Heparin
UFH binds to antithrombin and inactivates factor 10 and thrombin by forming a ternary complex
LMWH only inactivates factor 10 as it does not form this complex
Side effects: Immune induced thrombocytopenia, neurological injury
What clotting factors rely on the reduced form of Vitamin K?
Use and side effects of Warfarin?
7,9,10
Use: Prevents clotting after heart attacks
Side effects: Osteoporosis, bleeding, foetal haemorrhage
How does high levels of Aspirin increase the risk of a myocardial infarction?
COX 2 produces prostacyclin which switches platelets off and vasodilates; when this is blocked platelets are switched on and the vessels are vasoconstricted –> clots
How does Aspirin actually work?
Stops platelets from metabolising arachidonate acid to thromboxanes
Arachidonate acid is therefore metabolised to lipoxins which solve the response
What are ‘coxibs’
Example
COX 2 specific drugs
Celecoxib
4 side effects when Coxibs and ibuprofen are taken together
Hyponatraemia
Heohrotoxicity
Bleeding
Hyperkalaemia
What does ‘NO-NSAID’ stand for?
2 positive effects?
Nitric oxide-donating NSAID
Gastric protection and increased anti inflammatory effects
4 roles of Glucocorticoids
3 example drugs
Decrease inflammation caused by cytokines
Decrease prostaglandins and leukotrines
Decrease emigration of leukocytes from vessels
Increase apoptosis of lymphocytes and eosinophils
Hydrocortisone, Prednisolone, Dexamethasone
What are the three levels of steroid dose?
How is toxicity affected by these levels?
Topical: Low dose
Acute: Medium dose
Chronic: High dose
Higher dose = higher toxicity
Side effects of steroids (4)
Decreased response to infection
Decrease in steroid production
Carbohydrate and protein metabolism effects
Cushing’s syndrome
What do glucocorticoids inhibit?
Why does this lead to such a large effect?
Inhibit phospholipase A
Whole cascade is disrupted
2 examples of sedating antihistamines
2 examples of non-sedating antihistamines
How are non-sedating antihistamines different?
Chlorphenamine and Promethazine
Cetrizine and Fexofenadine
They decrease vascular permeability
What is the mechanism of Basilximab?
Pick up cytokine in blood and prevent it from binding OR bind to the receptor and prevent the cytokine from binding
Prevent proliferation by blocking JAK signalling
What is the mechanism of Cyclosporine and Tarcolimus?
Both bind to different primary molecules but then go on to block the same protein which is needed for dephosphorylation of a compound which activates IL2 transcription in the nucleus
IL2 activates T cells so without dephosphorylation, T cells are not activates
What is the mechanism for Rapamycin?
Blocks the protein mTOR which activates protein synthesis, cytoskeleton activation and migration of immune cells
Also blocks proliferation as mTOR also activates cyclins that help G1–>S phase in the cell cycle
What are DMARDs
5 examples
Disease modifying anti-rheumatic drugs
Methotrexate, Gold, Sulfasalazine, Penillamide, Chloroalanine
What does the drug Carbamazepine do?
What 2 things does it treat?
Increases the inactivated state of the sodium channel and refractory period
Treats nerve pain and epilepsy
What does Tetrodotoxin do?
What does it cause?
Blocks Na ion channels
Respiratory depression
What do local anaesthetics do?
Give 2 examples of esters and 3 examples of amides
Block sodium ion channels
Esters: Cocaine and Procaine
Amides: Lidocaine, Bupiracaine, Ropivacaine
What are the 4 classes of opioids?
e.g. of each
Natural e.g. morphine
Endogenous e.g. endorphin
Semi-synthetic e.g. heroin
Fully synthetic e.g. pethidine
When should you not give opioids?
Alcoholism
Respiratory depression
What receptors do opioids bind to in the brain?
Mu, Delta, Kappa
Side effects of opioids?
Constipation, drowsiness, hypotension, nausea, respiratory depression and vomiting
What are the roles of these 7 opioids? Morphine Sulphate Diamorphine (Heroin) Codeine Fentanyl Pethidine Tramadol
Morphine Sulphate: Most common
Diamorphine (Heroin): Increased power
Codeine: Mild-moderate relief, decreases cough and causes constipation
Fentanyl: Anaesthetic properties
Pethidine: Moderate-severe relief, obstetric and peri-operative
Tramadol: Decreases side effects by enhancing adrenergic and serotenergic pathways
What is the role of Naloxone?
An opioid receptor antagonist to reverse the effects of an opioid overdose
What drug is used to treat motor neurone disease?
What does it do?
Riluzole
Blocks glutamatergic neurotransmission to slow the progression of the disease
What is L-DOPA?
3 side effects?
Precursor of dopamine
Drug resistance, psychosis and involuntary movements
Side effect of a dopamine agonist?
Sleepiness
What is the treatment for Alzheimer’s - why?
3 examples of drugs
AChE inhibitors as there are decreased neurones in the hippocampus meaning ACh levels are reduced
Donepezil, Neostigmine, Physostigmine
What drugs do GABA receptors have binding sites for?
Benzodiazapines, Neurosteroids, Pricrotoxin, Barbiturates