Term
|
Definition
Antithyroid drug.
Inhibits thyroid peroxidase enzyme & blocks thyroid iodine trapping
Important S/E: BM suppression - agranulocytosis |
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Term
|
Definition
synthetic ADH analogue
Treatment of cranial diabetes insipidus
mimics ADH - increases water reabsorption at collecting duct
s/e: may cause dilutional hyponatraemia & fluid retention
other uses: used in water deprivation test to distinguish between cranial and nephrogenic DI. Vasopressin and terlopressin are used to control upper GI bleeding from varacies - desmopressin doesnt have vasoconstrictor properties and cannot be used for this! |
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Term
| Gliptins - e.g. sitagliptin |
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Definition
| DPP-4 inhibitor used in T2DM in combo with other oral hypoglycaemic agents - prevent breakdown of incretins - which increases stimulates insulin production from pancreas and decreases glucagon |
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Term
|
Definition
| increase insulin sensitivity in skeletal muscle, adipose tissue and liver via action on PPAR-gamma receptors |
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Term
|
Definition
Biguanide.
Acts as an insulin sensitising agent - does not increase insulin production.
common s/e: anorexia/wt loss - thus good in obese patients!
may cause lactic acidosis - especially with excess alcohol, renal/hepatic failure, severe dehydration, gen anaesthetic
stop metformin prior to contrast administration - prevent renal impairment. |
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Term
|
Definition
sulphonyurea - blocks ATP dependant K+ channels in beta cells of pancreas. Causes depolarisation, calcium influx and release of insulin
s/e: hypoglycaemia |
|
|
Term
Name two metals who's salts are used as antacids.
Which one causes diarrhoea as a s/e ?
and which one causes constipation? |
|
Definition
Magnesium salts cause diarrhoea
Aluminium salts cause constipation |
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Term
|
Definition
Is an antispasmodic - antimuscarinic
relax intestinal smooth muscle via acting on parasympathetic NS in gut
common side effects: dry mouth, constipation
contraindicated in MG and angle closure glaucoma |
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Term
|
Definition
aminosalyclate
maintenence therapy in UC (+ sometimes Crohn's) |
|
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Term
|
Definition
nucleotide analogue
used in chronic hepatitis B infection
Blocks reverse transcriptase required for hep B viral replication
Peginterferon alfa is the mainstay of tx. Adefovir is only used if the latter is contraindicated or poorly tolerated |
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Term
|
Definition
used in IBD and prevention of transplant rejection, GVHD
Calcineurin inhibitor - prevents proliferation of T lymphocytes - reduces cytokines particularily IL2
increased risk of secondary lymphomas caused by EBV |
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Term
|
Definition
H1 receptor antagonist in CTZ
can be used for labyrinthitis, motion sickness as well as N&V
safe in pregnancy |
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Term
|
Definition
H2 receptor antagonist
decreases gastric acid production by antagonising the effects of histamine at the membrane bound H2 receptors on gastric parietal cells.
exclude gastric cancer before prescribing to elderly patients as it may mask the symptoms |
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Term
|
Definition
Vitamin B12
needed for synthesis of nucleic acids - DNA
Given as Injections |
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Term
|
Definition
Osmotic laxitive
lactulose is a disaccaride of fructose and galactose. Cannot be metabolised by human enzymes, but is hydrolysed by colonic bacteria - where the products exert an osmotic effect in the colon. |
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Term
|
Definition
opioid antimotility drug
acts on mu opioid receptors in myenteric plexus of gut wall - prevents Ach release from myenteric plexus and hence peristalsis
doesnt cross BBB - hence less likelihood of dependance like other opioids |
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Term
|
Definition
dopamine antagonist - D2 receptors
blocks D2 receptors at CTZ
Increases gastric and duodenal emptying via relaxation of pyloric sphincter
may cause tardive dyskinesia. Increases the risk of extra pyramidal side effects of antipsychotic agents
Increases absorption of paracetamol - a nice wee combo for migraine |
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Term
| whats the difference between domperidone and metoclopramide ? |
|
Definition
domperidone doesnt cross BBB, metoclopramide does.
This makes domperidone suitable for treatment of nausea as a side effect of levodopa therapy without decreasing the dopaminergic effect in the brain (i.e. target) |
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Term
|
Definition
5-HT3 antagonist - i.e. serotonin
chemo & radiotherapy N&V
blocks 5HT3 receptors in CTZ and GI tract
can increase effect by adding dexamethasone |
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Term
|
Definition
PPI - dose dependant irreversible inhibition of gastric acid secretion - blocks H+/K+ ATPase pump
useful in GORD, part of H pylori eradication, zollinger-ellison syndrome, oesophagitis, GU or DU etc
Omeprazole is an enzyme inhibitor - thus increases plasma concentration of warfarin and phenytoin. |
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Term
|
Definition
stimulant laxitive
hydrolysed by colonic bacteria producing derivitives that are irritant to GI tract. These stimulate the myenteric plexus and increase peristalsis.
risk of atonic colon with prolonged use |
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Term
|
Definition
Dopamine agonist
D2 receptors
Parkinsons disease, acromegaly, hyperprolactinaemia (inhibits PRL from pituitary - and GH but only in acromegalics)
Domperidone useful in treating N&V side effect |
|
|
Term
Carbemazepine
give me 3 indications
what does it do to enzymes? Give me two interactions due to this |
|
Definition
anticonvulsant
generalised tonic clonic seizures, partial seizures, trigeminal neuralgia
enhances GABA inhibitory transmission in CNS
decrease electrical excitability via blocking sodium and calcium channels
enzyme inducer: reduces efficacy of OCP, reduces warfarin effects
can cause agranulocytosis |
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Term
|
Definition
| inhibits platelet aggregation via inhibition of phosphodiesterase - causing low intracellular Ca |
|
|
Term
| ethosuxamide - when would you use it? |
|
Definition
|
|
Term
| What does phenytoin do to liver enzymes ? |
|
Definition
|
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Term
|
Definition
Serotonin 5HT1 agonist
used in migraine
stimulates inhibitory 5HT1 receptors in raphe nucleus of brain - maintaining vasoconstrictor tone in carotid territory.
best given SC due to delayed gastric emptying in migraine and poor oral bioavailability. Take as soon as the pain starts. |
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Term
|
Definition
used in all types of epilepsy
increases GABA content of brain via inhibition of GABA transaminase enzyme
also blocks voltage gated sodium channels |
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Term
|
Definition
blocks voltage gates Na+ channels - stabilising neuronal thresholds against excitability. Prevents spread of epileptic discharges - not their initiation.
lots of s/e's including gum hypertrophy, steven johnsons, drug induced SLE, peripheral neuropathy
hepatic enzyme inducer - thus decreases OCP and warfarin effects
v narrow theraputic window
non linear relationship between dpse and plasma concentration - i.e. zero order kinetics |
|
|
Term
| Why give entacapone in PKD ? |
|
Definition
COMT inhibitor - can extent plasma t1/2 of L-dopa
useful for fluctuations in advanced PKD |
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Term
|
Definition
antibiotic
inhibits protein synthesis
used for bacterial eye infections - conjunctivitis |
|
|
Term
pilocarpine
what does it do to pupil ? |
|
Definition
muscarinic receptor agonist
acts theraputically at M3 receptor in acute angle closure glaucoma - causes ciliary muscle contraction - thus opens up trabecular meshwork allowing drainage of angle
constricts the pupil - miosis |
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Term
|
Definition
beta blocker
administered topically in glaucoma - decreases intraoccular pressure |
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|
Term
Dorzolamide
name another example of a drug in this group |
|
Definition
carbonic anhydrase inhibitor - decreases aqueous humour production - lowers intraoccular pressure in glaucoma
other example: acetazolamide |
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|
Term
Latanoprost
why would girls seek to buy this on the black market? |
|
Definition
prostaglandin analogue
increases outflow of aqueous humour - decreasing intraocullar pressure
side effect of eyelash growth ! |
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Term
|
Definition
amoxicillin and clavulanic acid
Binds to penicillin binding protein in bacterial cell wall - and prevents peptidoglycan cross linkage - inhibiting bacterial cell wall synthesis causing cell lysis
moxicillin is susceptible to degradation by β-lactamase-producing bacteria, and so may be given with clavulanic acid to increase its susceptability. |
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Term
|
Definition
benzodiazepine used in alcohol withdrawl
binds to stereospecific benzodiazepine (BZD) binding sites on GABA (A) receptor complexes at several sites within the central nervous system
GABA exerts an inhibitory effect on CNS via increased chloride influx - membrane hyperpolarisation (more difficult to depolarise!) |
|
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Term
|
Definition
| used in maintenance of alcohol abstinence |
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|
Term
Azathioprine
Name one important drug interaction.
how does this illustrate an example of pharmacogenetics ? |
|
Definition
is a prodrug - metabolised to 6 mercaptopurine in liver
purine analogue.
Its mechanism of action is likely due to incorporation of thiopurine analogues into the DNA structure, causing chain termination and cytotoxicity.
Thus with no DNA synthesis, the T cells cannot proliferate.
Finally metabolised by xanthine oxidase - thus dont give it with allopurinol !
mercaptopurine is deactivated by TPMT enzyme - for which genetic polymorphisms exist, thus genetic variability in how drug is handled |
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|
Term
Sulphasalazine
outline why this drug is a good example of targeting a specific site? |
|
Definition
Sulphapyridine and 5 aminosalicylic acid compound - deconjugated by colonic bacteria - meaning that mesalazine is delivered to the target tissues when used in IBD
the sulphapyridine group is the important bit in rx of RA |
|
|
Term
cabergoline
why does this drug illustrate the importance of investigating hormones involved in a pituitary adenoma ? |
|
Definition
dopamine agonist & prolactin inhibitor
microprolactinoma (with no mass effect) can be managed medically !! thus establishing a high PRL with no other hormone excess is important as the patient wont require surgery or dxt |
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|
Term
apomorphine
what will patients almost inevitably do when this is administered ?
how is it administered ? |
|
Definition
Powerful dopamine agonist - D1 and D2 receptors
patients will almost always vom !! must administer with domperidone if using in parkinsons disease
always given SC |
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Term
|
Definition
MAO-B inhibitor
monoamine oxidase breaks down dopamine - thus inhibiting this enzyme increases dopamine availability
useful in early parkinsons - esp younger patients - may delay progression and prevent levodopa therapy early on |
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Term
|
Definition
partial seizures in epilepsy and generalized seizures of Lennox-Gastaut syndrome
inhibits voltage-sensitive sodium channels and/or calcium channels, thereby stabilizing neuronal membranes and consequently modulating presynaptic transmitter release of excitatory amino acids |
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|
Term
beta interferon
can you think of any interesting health economics factoids ? |
|
Definition
used to reduce the rate of relapse and slow disease progression in MS
currently not recommended by NICE due to ICER > threshold (£/QALY). Currently available to patients via risk sharing scheme in UK - following dicussion with drug companies. Kind of a long term trial - as previous clinical data was too short term to be extrapolated. Drug companies have agreed to lower the price to NHS if scheme shows that cost effectiveness ICER is still too £++ |
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|
Term
tamsulosin
name another drug in this class. |
|
Definition
Tamsulosin is a selective antagonist at alpha-1A and alpha-1B-adrenoceptors in the prostate, prostatic capsule, prostatic urethra, and bladder neck
Blockage of these receptors causes relaxation of smooth muscles in the bladder neck and prostate, and thus decreases urinary outflow resistance in men.
doxazosin |
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|
Term
trimethoprim
what should you not co prescribe?
Why dont you get similar side effects as drug above?
why should you avoid this drug in pregnancy ? |
|
Definition
inhibits dihydrofolate reductase - prevents bacterial thymidine and thus DNA synthesis
Methotrexate !! also inhibits dihydrofolate reductase
trimethoprim has a much higher affinity for bacterial dihydrofolate reductase then mtx - which prefers the human enzyme
antifolates are not a good idea in pregnancy .... |
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|
Term
finasteride
what might this do to a bald man ? |
|
Definition
testosterone 5-alpha-reductase inhibitor
used in tx of BPH
blocks the peripheral conversion of testosterone to DHT, resulting in significant decreases in serum and tissue DHT concentrations
DHT is responsible for prostatic growth, thus lowered levels of this decrease prostatic volume
increase hair regrowth and decrease hair loss! |
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Term
|
Definition
loop diuretic
acts on thick ascending limb at Na-K-2CL cotransporter
prevents Chloride from binding - thus prevents sodium reabsorption - causing the interstitium to be less hypertonic - preventing absorption of water along osmotic gradient |
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|
Term
|
Definition
thiazide diuretic
prevents Na-Cl co transporter action
can cause hypokalaemia via an increase in sodium-potassium exchange mechanism - thus increased excretion of potassium |
|
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Term
|
Definition
COCP
decreases acne and hirsutism in PCOS |
|
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Term
|
Definition
|
|
Term
Levothyroxine
where is the receptor that it acts upon? |
|
Definition
T4 !
thyroid hormone receptor is in the nucleus and cytoplasm - intracellular ! |
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Term
|
Definition
synthetic mineralocorticoid
acts like aldosterone
given in Addisons disease that is due to atrophy of adrenal glands. Doesnt need to be given if ACTH is diminished but adrenals are intact - as aldosterone remains under control of renin-angiotensin-aldosterone system |
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Term
|
Definition
|
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Term
|
Definition
|
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Term
|
Definition
|
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Term
|
Definition
|
|
Term
acyclovir
in what way is the action of this drug specific to target ? |
|
Definition
antiviral agent - used in herpes simplex and herpes zoster infections (not ok in CMV!)
converted by *viral thymidine kinase* - thus inhibitng viral DNA polymerase
latently infected cells are not affected |
|
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Term
|
Definition
tamiflu !
used for influenza viruses - prevents release and spread of virus
does this by inhibiting neuraminidase |
|
|
Term
| outline the 5 main classes of antiretroviral drugs |
|
Definition
1. nucleoside reverse transcriptase inhibitors (NRTIs)
2. non nucleoside reverse transcriptase inhibitors (NNRTi's)
3. Protease inhibitors
4. fusion and entry inhibitors
5. integrase inhibitors |
|
|
Term
| name a long acting insulin |
|
Definition
|
|
Term
| name a short acting insulin |
|
Definition
|
|
Term
| give an example of a mixed insulin preparation |
|
Definition
|
|
Term
| Outline a H pylori eradication regime |
|
Definition
Confirm presence of H pylori prior to regime
PPI + clarithromycin + amoxicillin/metronidazole
if unsuccessful - need to do culture and sensitivity due to resistance |
|
|
Term
| outline one non genomic effect of corticosteroids in inflammation |
|
Definition
| release of annexin-1 - prevents activity of phospholipase A2 - prevents cleavage of phospholipid membrane & formation of arachadonic acid (and thus its downstream eicosanoids molecules leukotrines, prostaglandins) |
|
|
Term
| Name 4 hepatic enzyme inducers |
|
Definition
Phenytoin
Carbamazepine
Rifampicin
St Johns Wort |
|
|
Term
| Name three hepatic enzyme inhibitors |
|
Definition
erythromycin
Quinine
Ciprofloxacin |
|
|
Term
| why might orlistat affect INR ? |
|
Definition
| orlistat inhibits pancreatic lipase - vitamin K is a lipid soluble vitamin - thus if there is less fat absorption - there will be less absorption of vitamin K and warfarin has less substrate - thus INR +++ |
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|
Term
| Which antibiotic causes acute hypersensitivity to alcohol ? (disulfram reaction) |
|
Definition
|
|
Term
| What antibiotic causes yellow staining of teeth ? |
|
Definition
|
|
Term
|
Definition
| gastroprotective agent. PGE1 analogue - increases gastric mucus secretion and inhibits acid secretion (kind of undoes the bad things NSAIDS do in the stomach) |
|
|
Term
what does erythromycin do in stomach ?
What condition might this be useful in ? |
|
Definition
Binds to motilin receptor and enhances gastric emptying
useful in gastroparesis e.g. in diabetic autonomic neuropathy |
|
|
Term
| why give levodopa and not dopamine ? |
|
Definition
| dopamine is poorly lipid soluble, has poor oral absorption and does not cross BBB (L-dopa is transported across using amino acid transport) |
|
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Term
|
Definition
produced by C cells in thyroid gland - reduces serum calcium when high - the opposite of PTH
inhibits absorption from GI tract
inhibits osteoclasts |
|
|
Term
| Gs-alpha activates what ? |
|
Definition
| adenylate cyclase --> cAMP increase --> protein kinase A |
|
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Term
| Gq-alpha activates what ? |
|
Definition
Phospholipase C
causes: increase in IP3 activates protein kinase C via calcium release
DAG binds and activates protein kinase C directly
optimal activation of protein kinase C needs DAG and Ca (via IP3) |
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Term
|
Definition
used to treat malignant hypertension
acts as a nitric oxide donor, instatntly relaxes vascular smooth muscle |
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Term
|
Definition
NSAID - used to treat nephrogenic diabetes insipidous
inhibits PG synthesis, thus increasing cAMP in collecting duct, increasing water reabsorption (normally prostaglandins reduce action of ADH at kidney) |
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