Pharmacology Flashcards
What is Azathioprine and what is it used for?
An immunosuppressant used in IBD
What are the 5 mechanisms of drug resistance?
Drug inactivators (b lactam -> penicilloic acid) Decreased accumulation (pumped back out) Altered binding site Alternative pathways Chromosomal mutation
Why should antacids not be taken with other oral drugs?
Decreased acidic environment leads to risk of malabsorption.
Name a PGE2 analogue
Misoprostol
What is sulcrafate and what is an example brand name?
Gel former at low pH (protects mucosa AND BUFFERS ACID) eg Gaviscon
What are the four types of malarial plasmodium and which is the nastiest?
Falciparum (most nasty), vivax/ovale and malariae
Which tetracycline antibiotic is used in mefloquine-resistant malaria?
Doxycycline
Which is the only liver schizonticide?
Primaquine
Which antimotility drug is the main one used for diarrhoea?
Loperamide
Which four areas of medications most commonly cause constipation?
Narcotics,
Diuretics
Anti epileptics
Antispasmodics
Name four diseases that often lead to constipation
MS, Parkinson’s, Stroke, Diabetes
In which organelle are the main drug-metabolising enzymes found?
Smooth ER
What are the two phases of drug metabolism? (With aim of increasing water solubility)
1 - Oxidation, Reduction, Hydrolysis (metabolites usually inactive, frequently undergo phase 2)
2 - Conjugation (metabolites almost always inactive -> excreted)
What is the treatment for C.diff?
Stop unnecessary ABs and start on Metronidazole or Vancomycin
Name the two PDIs used in Parkinson’s
Benserazide and Carbidopa
Name two general anaesthetics used for induction (rapid onset, short action, IV)
Thiopentone and propofol
Name two general anaesthetics used for maintenance (inhaled, slow onset)
Nitrous oxide, Isoflurane
How do NDMRs have their effect? And name one.
Non-depolarising Muscle Relaxants:
NMJ transmission by binding competitively at nACh-R
Tubocuraine
What effect does ketamine induce, and how does it do it?
Analgesia and paralysis with loss of consciousness, through NMDA-R antagonism.
What is a drug that decreases GABA function termed? And what effect do they have?
Benzodiazepine receptor inverse agonist = potent convulsants
Name the three subtypes of NSAIDs and give an example drug of each.
Salicylic acids (Aspirin), Propionic acids (Ibuprofen) and Acetic acids (Indometacin)
Which process normally leads to fever after bacterial infection, which NSAIDs can block?
Bacterial endotoxins usually increase PGE1 in the hypothalamus which increases temperature set-point.
Name 6 NSAIDs and identify which are the most COX-1 and COX-2 selective
Piroxicam (COX-1) Indometacin Naproxen Aspirin Ibuprofen Rofecoxib (COX-2)
Name a NSAID and a 5HT antagonist used in migraine.
NSAID - Tolfenamic acid
5HT antagonist - sumatriptan
Name an antimuscarinic used in NV.
Hyoscine
Name two antihistamines used in NV
Cyclizine and Promethazine
Name the NK1-R antagonist used as an adjunct in antiemetic treatment with chemo
Aprepitant
What is clavulanic acid?
A b-lactamase inhibitor given WITH antibiotics to overcome resistance (NOT an AB itself!)
How do 5HT agonists (triptans) help treat migraine?
Inhibit trigeminal nerve transmission and co strict vascular smooth muscle
What is the active metabolite of omeprazole?
Sulphenamide
What happens in aspirin overdose?
Salicylism (tinnitus, vertigo, vomiting) and resp and met acidosis
What is Reye’s syndrome? Which drug is it associated with?
Encephalopathy and liver damage, under 12 years of age, associated with aspirin use
Name an anti-TNF used in Crohn’s
Infliximab
What are the 3 categories of broad-spectrum antibiotics?
Tetracyclines, Carbapenems and Cephalosporins
What condition is Primaquine contraindicated with?
G6PD deficiency
Name 4 TCAs
Amitriptyline
Lofepramine
Clomipramine
Imipramine
Name the main serotonin-NA reuptake inhibitor in antidepressants
Venlafaxine
Name two MAOIs
Phenelzine
Moclobemide
What enzyme do Proguanil and Pyrimethamine inhibit?
Plasmodium Dihydrofolate Reductase
Which drug is Proguanil combined with to make Malarone?
Atovaquone
What is the basic structure of a local anaesthetic?
Aromatic (lipid soluble) — Ester/Amide — Amine (water soluble)
Which is the most commonly used local anaesthetic?
Lidocaine
What are the 5 main side effects of opioids?
Respiratory depression Nausea and vomiting Cough suppression Miosis Constipation
Name the first and second line rapid acting blood schizonticides
Chloroquine and Mefloquine
Name 3 dopamine antagonists used in NV
Metoclopramide
Droperidol
Domperidone
What receptor do triptans act on?
And what condition is sumatriptan use to treat?
5HT antagonists
Migraine
What are the 3 main antifungals and what are they each used for?
Fluconazole and itraconazole (both triazoles) - candida
Amphotericin (polyene) - IV for systemic fungal infection
What is the suffix for all 5-ASA anti inflammatory drugs used in IBD? And which is the only one used in Crohn’s as well as UC?
-salazine
Sulfasalazine
What are four drugs given as prophylaxis for migraine?
Propranolol (b-blocker) Topiramate Gabapentin (both antiepileptics) Pizotifen (5HT Antagonist) (Also TCAs)
Name 3 anti-virals used in HIV
Enfurvitide, Zidovudine and Indinavir
Name a CA inhibitor used in glaucoma and describe why it works?
Acetozolamide - decreases intraocular pressure by decreasing aqueous production by ciliary epithelium
The co administration of which drug with paracetamol can protect against the liver damage caused by its toxic metabolite?
Methionine
Name an adsorbant used in diarrhoea and the cases in which it would be used?
Kaolin, following colostomy/iliostomy or diverticular disease
Name 3 anti-motility opiates used in diarrhoea
Cophenotrope,
Loperamide
Codeine
Name 3 anti-muscarinics used in diarrhoea and how they work
Atropine, Propanthelone, Dicycloverine
Antispasmodics that block PNS action on myenteric and submucosal plexuses
What receptor does Ondansetron act on? Name 3 S/Es
5HT3 in the CTZ
Constipation, flushing, headache
Name 2 antihistamines used in nausea/vomiting
Cyclizine
Promethazine
What receptor does Hyoscine act upon?
Muscarinic
Name 3 non-phenothiazine neuroleptics
Haloperidol
Flupenthixol
Pimozide
Name 3 phenothiazine neuroleptics and the main S/Es of Group 1 and 2
Chlorpromazine - sedation
Pipothiazine - antimuscarinic
Fluphenozine
What are the S/E of D2 antagonist neuroleptics associated with the hypothalamus?
Pituitary hormone release alteration:
Increased prolactin -> sexual dysfunction
Increased cortisol -> Cushing’s
Decreased GH
Name the 2 atypical neuroleptics with the fewest S/Es
Risperidone and Sulpiride
Which enzyme do Imidazoles and Triazoles inhibit?
Lanosterol Demethylase
Name 3 triazole antifungals
Fluconazole, Itraconazole, Variconazole
How do polyenes work? Name 2
Generate membrane pores,
Amphotericin and Nystatin
What is the active metabolite of Carbamazepine?
Eslicarbazepine
Which anti-epileptic has the most S/Es?
Phenytoin
Name the NMDA antagonist antiepileptic
Topiramate
Name a GABA antagonist that will cause convulsions
Picrotoxin
Name 4 drugs for tonic-clonic epilepsy and 3 add-on drugs
Sodium Valproate, Lamotrigine, Carbamazepine, Clonazepam
Add-on: Gabapentin, Pregabalin, Vigabatrin
Name 2 anti virals used against Influenza
Amantadine, Oseltamivir
Which DNA bases are each of the nucleic acid inhibitor anti virals analogues for?
Acyclovir - guanosine
Zidovudine - thymidine
What are the S/Es of zidovudine?
Anaemia, bone marrow suppression and liver toxicity
What are the S/Es of amantadine?
CNS dopaminergic - nervousness, anxiety, insomnia
What are the S/Es of indinavir?
Kidney stones, hyperlipidaemia
Name 2 antimuscarinics used as adjunct for tremor and rigidity in Parkinson’s
Benzhexol and Procyclidine
Name 2 selective and 1 non-selective DA agonist used in Parkinson’s
Bromocriptine and Lysuride
Apomorphine
Name 3 osmotics and 2 softeners used in constipation
Osmotics - Lactulose, Macrogols, Mg salts
Softeners - Docusate, Arachis oil
Name 2 bowel cleansers used before surgery and radiology
Sodium acid phosphate
Sodium picosulphate
Name 3 stimulants used in constipation and the S/Es
Bisacodyl, Dantron, Senna
S/E- cramp, diarrhoea, tolerance
Outline the 3 categories of anxiolytic/hypnotic drugs and name 2 drugs in each.
Barbiturates - phenobarbital, thiopental
Benzodiazepines - diazepam, clonazepam
Z drugs - zopiclone, zaleplom
Name 2 anxiolytic drugs given IV as anaesthetic pre-medication
Diazepam
Lorazepam
Name 2 rapid and 2 slow acting blood schizonticides
Rapid - Chloroquine, Mefloquine
Slow - Proguanil, Pyrimethamine
What is the name for pyrimathamine a) + dapson and b) + sulfadoxine?
+ dapson - Maloprim
+ sulfadoxine - Fansidar
Name the three groups of Monoamine Reuptake Inhibitors used as antidepressants and name 2 drugs of each
SSRI - Fluoxetine, Citalopram
Serotonin-NA RI - Venlafaxine, Duloxetine
TCA - Amitryptaline, Imipramine
What is Agomelatine?
A melatonin-receptor agonist and 5HT2 antagonist used in depression
Name an antidepressant that acts as an autoreceptor antagonist
Mirtazapine
Name 2 Streptogramins
Quinupristin
Dalfopristin
Which enzyme do Sulphonamides inhibit?
And which does Trimethoprim inhibit?
Dihydropteroate Synthase
Dihydrofolate Reductase
What is the active metabolite of Azathioprine?
Mercaptopurine
Which opioid antagonist is given for acute opioid overdose?
Naloxone
Which type of patient must NOT be given PGE analogues?
Pregnant - spontaneous abortion
