Pharmacology Flashcards
6 pharmacological considerations for any drug
Pharmacokinetics Dosage Administration Accumulation in tissues and organs Toxicity Interference with other drugs
Give 4 examples of antibiotic classes which can be used to inhibit protein synthesis
30s inhibitors
50s inhibitors
tRNA inhibitor
EF-G elongation factor protein
Give 2 antibiotic classes which are 30s inhibitors
Give 1 example of a drug in each class
Aminoglycosides e.g. gentamycin
Tetracyclines e.g. oxytetracycline
What is special about the mechanism of action of tetracyclines?
They also cause host toxicity but are more potent in bacteria so at the right dose they can be used to kill bacteria
Give 2 antibiotic classes which are 50s inhibitors Give 1 example of a drug in each class Give the name of 2 other 50s inhibitors
Macrolides e.g. erythromycin
Lincosamide e.g. cindamycin
chloramphenicol
oxazolidinoes
Give 2 examples of drugs which are tRNA inhibitors
Puromycin
Mupirocin
Give 1 example of a drug which is an EF-G elongation factor protein
Fusidic acid
Give 3 examples of antibiotic classes which inhibit cell wall synthesis
What specifically do they inhibit
Beta lactam
Glycopeptides
Cephlasporins
Peptidoglycan
Explain the MOA of Beta lactam antibiotics
Give 2 examples of drugs
Inhibit penicillin binding proteins to prevent cross linking
Penicillin, Amoxicillin
Explain the MOA of Glycopeptides What bacterium do they work on Give an example of the drug class and 1 drug
Binds to the cell wall subunit to stop cross linking
Gram positive
Macrolides e.g. erythromycin
Give an example of a cephlosporin antibiotic
Cefradine
Give 3 examples of antibiotic classes which work on the metabolic pathway
Sulphonamides
Trimethoprom
Fosfomycin
Explain how THFA is produced in eukaryotes and prokaryotes
Why is it needed?
Tettrahydrofolic acid is a precursor to nucleic acid
Eukaryotes: DHR taken up > THFA
Prokaryotes: Dihydrofolic acid > DHR > THFA
Explain the MOA of sulphonamides
Give 1 example
Stops dihydrofolic acid production
Sulfamathozazole
Explain the MOA of trimethoprim
Why does it not affect humans?
Structural analogue of folic acid so stops dihydrofolic acid production
It has an increased potency in bacteria
Explain the MOA of fosfomycin
What is is often used for?
Is it broad or narrow spec?
A metabolic analogue which inhibits cell wall synthesis
Used in the kidney and bladder
Broad spectrum
Give 2 examples of antibiotic classes that target nucleic acids
Quinolones
Rifamycins
MOA of Quinolones
2 examples of drug classes and 1 example of a drug
Inhibit DNA replication
Gyrases
Topoisomerases e.g. ciprofloxacin
MOA of Rifamycins
1 example of a drug
Block mRNA synthesis
Rifampicin
Give 2 examples of drugs which act on the cytoplsmic membrane
MOA?
Clinical use?
Polymixins
Colistin
Act as a detergent on the membrane
Rarely used due to topical toxicity but increasing due to resistance of other antibiotics
2 examples of Neuraminase inhibitors
Which virus are they often used for?
Ostltamivir (Tamiflu) and Zanamivir
Influenza
3 examples of nucleotide analogues
2 viruses they are often used for
Acivlovir (Zovirax), Valaciclovir, Famciclovir
Herpes simplex and Varicella Zoster
4 examples of DNA polymerase inhibitors
Which virus are they often used for?
Ganciclovir, Vaganciclovir, Cidofovir, Foscarnet
CMV
1 example of an RNA polymerase inhibitor
2 viruses it is often used for
Ribavirin
RSV and Lassa Fever
What is the MOA of Leter movir
2 viruses it is often used for
Inhibits regulation causing overreplication
Adenovirus and VZV
What drug is used to treat Hepatitis C?
When are they used?
Protease inhibitors (-previr/-asvir/-buvir) In the first 8-16 weeks
What does aspirin block?
Cyclo-oxygenase pathway
What do corticosteroids block
Arachidonic acid release
Give 6 examples of drug classes used to treat HIV
Nucleoside reverse transcriptase inhibitors (NRTI’s)
Non-nucleoside reverse transcriptase inhibitors (NNRTI’s)
Protease inhibitors (PI’s)
Boosting agents (boost PI’s)
CCR5 inhibitors
Integrase inhibitors
Give 4 examples of Nucleoside reverse transcriptase inhibitors (NRTI’s)
Abacavir, Tenofovir, Lamiwdine, Emtricitabine
Give 4 examples of Non-nucleoside reverse transcriptase inhibitors (NNRTI’s)
Neviraphine, Efavirenz, Etravirine, Rilpivime
Give 2 examples of Protease inhibitors (PI’s)
Atazanavir, Darunavir
Give 2 examples of Boosting agents (boost PI’s)
Ritonavir, Cobicistat
Give an example of a CCR5 inhibitor
Maraviroc
Give 3 examples of Integrase inhibitors
Raltegravir, Elvitegravir, Dolutegravir
What drugs is given for PrEP
Truvada
Tenofovir and Emtricitabine
90-90-90
90% diagnosed
90% on treatment
90% virally surpressed
Give 4 examples of antifungal drugs
Amphotericin
Echinocandins
Flucanazole / Voricanazole
What spectrum is Amphotericin?
What is it toxic to and how is toxicity decreased?
Broad spectrum
Toxic –> fever and renal damage
Lipid formulations decrease toxicity
MOA of Echinocandins
What are the resistance patterns?
What is it used to treat? (2)
Inhibits glucan synthesis in the cell wall
Resistance emerging
Aspergillious and Candida albicans
MOA of Flucanazole / Voricanazole
2 problems
Inhibits ergosteral biosynthesis (unique to fungi)
Liver damage
Resistance to candida (not to the others)
3 drugs used to treat malaria
Quinolones
Anti-folats
Artemisin compounds
MOA of Quinolones
Example
Parasite uses Hb for proteins but needs to breakdown haem
Drug stops the breakdown of haem causing toxicity
Chloroquine
MOA of anti-folates
Folic acid metabolism is needed for DNA synthesis
MOA of artemisin compounds
3 benefits of this drug
Generate free radicals which attack proteins and lipids in the infected RBC
Reduces gametocyte carriage
Rapid, well-tolerated, low resistance
5 drugs used for the treatment of African Tyranosomiasis
Pentamidine, Suramin, Melarsoprol, Eflounithine, Niltfurtimox
2 drugs used in the treatment of South American Tyranosomiasis
Do they cure the disease?
Benznidazole and Niltfurimox
The disease is uncurable (lifelong)
3 drugs used in the treatment of Leishmaniasis
Pentavalent antimony, Amphotericin B, Milefosine
What drug is used in the treatment of Toxoplasmosis
Pyrimethamine
3 drugs used in the treatment of intestinal protozoans
Metronidazole, Tinidazol, Nitazoxanine
Give 3 drugs used in the treatment of helminths
What helminth are they used for?
Praziquarviel (schistomiasis)
Mebendazole (roundworms)
Albenazole (tapeworms)
What are the two MOA of methotrexate? (for cancer therapy)
Inhibit purine synthesis
Inhibit DTMP synthesis
Give 2 examples of drugs which inhibit DTMP synthesis
What are they used in the treatment of?
Methotrexate, Fluorouracil
Chemotherapy drugs for cancer
What is the MOA of cisplatin?
Alkylating agent
Cross-links DNA
What is the MOA of doxorubin?
What is it used in the treatment of?
Inhibits RNA synthesis
Chemotherapy drug for cancer
Give 3 examples of drugs which can be used to reverse cytotoxic drug resistance by drug efflux?
Verapamil
Quitidine
Cyclosporine
Give 3 examples of tyrosine kinase inhibitors
What mutation are they used for?
Gefitinib, Erlotinib, Osimertinib
EGFR mutations
What drug is used to overcome resistance to Gefitinib?
How is resistance caused?
Rocitetinib
A secondary mutation ‘spits’ out Gefitinib
What drug is used in people who have CML caused by a mutation in the Philadelphia chromosome?
Imatinib
What drug is used in people with melanoma caused by the BRAF gene?
Vemurafenib
Odbrafenib
What drug is used in people with breast/gastric cancer caused by the HER2 gene?
Trastuzumab
What drug is used in people with colorectal cancer caused by the RAS gene?
Cetuximab
Give an example of a drug used to block angiogenesis
2 side effects
Nintendaib
Toxicity and blood pressure problems
Define steady state
Equilibrium at the end of a set number of administrations of a drug
Define xenobiotics
How does its effect differ?
A chemical compound which is foreign to to a given biological system (e.g. drug)
Different effects on different people
Name two drugs which cause ototoxicity
Gentamicin (aminoglycoside)
Loop diuretics
Explain the MOA of carbonic anhydrase inhibitors
Give an example
Blocks carbonic anhydrase in the PCT to decrease the production of H+
Decreased H+ excreted in exchange for Na+ means increased Na+ in the tubule
e.g. Acetazolamide
3 uses of D.Mannitol
Decrease intracranial pressure (before surgery)
Decrease intraocular pressure
Treatment of cerebral oedema in diabetics
2 examples of Loop diuretics
Explain the MOA
What do you need to monitor when using them?
Furosemide, Bumetanide
Block Na/K/2Cl transporter
Electrolyte, K and Na levels
Explain the MOA of thiazide diuretics
How long do the drugs last?
Decreases Na reabsorption at the Na/Cl (K) transporter in the DCT
Effect up to 12-24 hours
Which diuretics are the most potent and which are the least? (3)
Most: Loop
Middle: Thiazide
Least: Carbonic anhydrase
Give two examples of potassium sparing diuretics
Amiloride
Spironolactone
Explain the MOA of Amiloride
Inhibits Na reabsorption in the DCT and CD at the Na/K exchanger
Explain the MOA of Spironolactone
An aldosterone antagonist so works on the DCT and CD to increase sodium and water excretion
Why are potassium sparing diuretics needed?
If you block Na absorption across the tubule by other diuretics, there will be more Na reaching the Na/K pump in the CD so Na will be reabsorbed here and K will be lost
2 examples of when aldosterone antagonists should not be used
ACE inhibitor (can cause hyperkalaemia) Danger with drugs which may impair K secretion
2 drug classes which can be used for urinary symptoms
Alpha blockers
5-alpha reductase inhibitors
4 drugs used to treat stress incontience
Alpha adrenergic agonists
Tricyclic antidepressants
Duloxetine
Oestrogens
3 drugs used to treat an overactive bladder
Anticholinergics
Meribagion
Botox (tightens bladder)
5 antibiotics used to treat child UTIs
Which are used for lower and upper?
Lower: Amoxicilin, Trimethoprim, Cephalexin
Upper: Cefotaxmine, Gentamicin
Give 2 examples of drugs containing synthetic oxytocin
Syntocinon
Syntometrin
2 oral drugs used for labour analgesia
Paracetamol and Codeine
MOA of entenox
Blocks pain receptors and relaxes
6 stages of the pain ladder for pregnant women
Paracetamol - Codeine - NSAID - Tramadol - Amitryptiline - Opiates
3 stages of drugs (5) used for the treatment of nausea and vomiting in pregnant women
- Cyclizine/Promethazine
- Metaclopramide/ Peochlorperazine
- Ondanestron
4 treatments for Hyperemesis Gravidarum
Thiamine to prevent Wernicke’s encephalopathy
Pyridoxine and corticosteroids
Consider ondanestron
Top 4 antibiotics used during pregnancy
Penicillin - Cephlasporin - Erythromycin - Trimethoprim
How do you treat the pain in osteoarthritis?
What drug do you need to take alongside this
NSAIDs (need PPIs)
What is the MOA of nitrogen containing bisphosphonates
Give 1 example of a drug
Inhibit ATP intracellular enzymes
e.g. Alendronate
What is the MOA of non-nitrogen containing bisphosphonates
Give 1 example of a drug
Inhibits post translational modifications of GTP binding proteins needed for the actin cytoskeleton and osteoclast sealing
Some proteins also allow osteoclast precursor proliferation
e.g. Etidronate
What are the 5 main roles of bisphosphonates?
Osteoclasts: Inhibition, Decrease progenitor, Apoptosis
Osteoblasts: Increase function
When osteoclasts absorb bone with bisphosphonate attached it impairs the osteoclasts function
Give 2 examples of SERMs
Tamoxifen
Raloxifene
Give 4 examples of NSAIDs
Ibuprofen, Paracetamol, Diclofenac, Naproxen
MOA of methotrexate (2)
Cancer: Interferes with dihydrofolate reductase and cancer cell division
RA: Dampens the immune system
Side effect of sulphasalazine
What 2 diseases is it used to treat?
Reduces sperm count
Crohn’s and RA
MOA of hydrochloroquine in RA
Changes antigen presentation and effects on the innate immune system
What are the 3 biological therapies which can be used to treat RA?
Adamilumab, Etanercept, Infliximab
What is the MOA of biological therapies to treat RA?
Inhibits cytokines, TNF-alpha and the inflammatory cascade
Human IgG and variable region binding to TNF-alpha
4 problems with biologic therapies for RA treatment?
Expensive
Unstable
Need to be injected in hospital
Only work if the rheumatoid is in the active phase
Give 2 examples of immunosupressants used for RA therapy
How do they work?
Cyclophosphamide
Ciclosporin
Reduces the immune response and slows erosion
Decreases blood cell number
Give 5 examples of drugs use to treat glaucoma
How do they work?
Muscarinic antagonists (increase trabecular outflow) Prostaglandin antagonists (increase uveoscleral outflow) Beta blockers, A2 adrenorecpeotr agonists and Carbonic anhydrase inhibitors (reduce aq humour inflow)
What drugs are given to people in AF to reduce their risk of stroke?
Anticoagulants (massively decreases risk) e.g. Docac
Aspirin (slightly decreases risk)
Anti-platelet therapy e.g. Clopidogrel
What medication is given after a hemorrhagic stroke?
Anti-hypertensives
What medication is given after an ischaemic stroke?
Statin
Anti-platelet e.g. Clopidogrel
Anti-hypertensives
How do you acutely treat an infarct stroke?
Thrombolysis/Thrombectomy (patient may bleed)
Further treatment with Aspirin and Statin
How do you acutely treat a haemorrhagic stroke?
Severely lower blood pressure and stop anticoagulation
What are the 2 drugs used to treat Alzheimer’s
Give examples
AchE inhibitors e.g. Donepezil, Rivastigmine, Galantamine
NMDA antagonist e.g. Memantine
4 side effects and 4 cautions of AchE inhibitors
Side effects: Headache, nausea, vomiting, diarrhoea
Cautions: Asthma, peptic ulcer, seizure, arrhythmia
What is the MOA of Memantine?
Blocks the effect of increased glutamate
5 side effects and 1 caution of Memantine
Side effects: Dizzy, headache, constipation, sembalance, SOB
Caution: seizure
2 drugs to treat dementia with Lewy bodies
Which is preferable - why?
AchE inhibitor (doesn't always work but better tolerated) Antipsychotic
4 drugs used for epilepsy treatment
Sodium valoprate
Lamotrigine
Levetiracetam
Topiramate
5 drugs used for partial seizure treatment
Carbamazepine Zonisamide Lacosamide Perampanel (and anti-epileptic drugs)
What are the 2 classes of inhalational anaesthetics?
5 examples
Gas: NO, Cyclopropane
Liquid: IsoFLURANE, Halothane, Ether
What are the 3 classes of intravenous anaesthetics?
4 examples
Inducing agents: Propofol, Thiopentane
Dissociative anaesthesia: Ketamine
Neurolept analgesia: Fentanyl
Side effect of NO
Bone marrow supression
Side effect of ether
Malignant hyperprexia
What is the MOA of local anaesthetic?
Block voltage gated Na channels in all excitable tissue
2 examples of local anaesthetic
Esters/Amides
MOA of depolarising NMJ blocking drugs
Why do they have a short duration?
Why do they cause bradycardia?
What ion does it affect?
2 Ach molecules bound together binds to receptor
AchE breaks it down
Also slightly blocks muscarinic (parasympathetic) sites
K efflux
2 examples of depolarising NMJ blocking drugs
Suxamethonium
Succinylcholine
MOA of non depolarising NMJ blocking drugs
2 benefits
Competes with Ach preventing binding
Does not cause fasiculation or K efflux
3 examples of non-depolarising NMJ blocking drugs
- curonium
- curium
- curarine
Give 2 examples of AchE inhibitors
6 effects
Pyrdo/Neo stigmine
Bradycardia, GI peristalsis, Stops breathing, Hypersalivation, Bronchial secretions, Organophosphate poisoning
What is the antidote for AchE inhibitors?
What is its MOA?
Atropine
Blocks the parasympathetic system
Side effect of bisphosphonates
Gastric problems
Give an example of a drug to replace PTH
MOA?
Interaction?
Teriparatide
Increases osteoblasts
Interacts with bisphosphnates
What is the trade name for Densumab
What is its MOA?
Prolia
Mooclonal antibody to treat osteoporosis
Who does HRT cause problems in?
Problems in people who have opposed oestrogens as increased dementia, breast cancer and CVD risk
Less problems in people with unopposed oedtrogens (had a hysterectomy)
What is the effectiveness of the 4 main osteoporosis drugs?
Bisphosphonates = 30% Teriparatide = 70% vertebrae and 40% non (expensive) Prolia = 70% vertebrae, 40% hip, 20% other (expensive) HRT = 20-30%