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30 Cards in this Set
- Front
- Back
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What 2 things are needed in a ligand for the receptor to bind it |
Specific three dimensional topography and chemistry |
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What causes unwanted side effects |
The binding of a drug to multiple different types of receptors |
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What makes an ideal drug |
High potency and high specificity |
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What form of thalidomide is teratogenic and what is that |
R-Form and it’s an agent that disturbs the development of an embryo or foetus |
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What can thalidomide be used to treat |
Leprosy |
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What are the differences between r form and a form adrenaline/epinephrine |
R-form binds to 3 domains on the receptor, an anionic site, hydrogen bonding site and the flat area (3 bonds) has a better fit so is more active. S-form binds to 2 domains, the anionic site and the flat area (3 bonds) and so fits less and is less active than the R-form. |
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Acetylcholine receptors |
Nicotine and muscarinic |
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Nicotinic receptor |
Skeletal muscle, ganglia, CNS Ligand gated ion channel Excitatory Agonists are acetylcholine and nicotine Antagonists are tubocurarine and atracurium |
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Muscarinic receptor |
Widely distributed G-protein coupled receptors M1-M5 subtypes M1, M3 And M5 are PLC coupled receptors (Gq) M2 and M4 are cAMP couples receptors (Gi/o) Agonists are acetylcholine, muscadine and bethanocol Antagonists are atropine and hyoscine |
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Noradrenaline receptors |
a(alpha) adrenoreceptors and b(beta) adrenoreceptors |
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a (alpha) adrenoreceptors |
Widely distributed GPCRs a1 (PLC coupled) and a2(cAMP coupled) subunits Agonists are adrenaline and noradrenaline Antagonists are phenoxybenzamine and phentolamine |
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B(beta) adrenoreceptors |
Widely distributed GPCRs B1, B2 And B3 are adenylate Cyclades activated cAMP-PKA B2 (Gi) cAMP coupled Agonists are adrenaline and noradrenaline Antagonists are propanalol and sotalol |
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False transmitters |
Mimic/replace NA Alpha-methyldopa Guanethidine |
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Alpha-methyldopa |
Used for hypertension (high blood pressure) Inhibits dopamine synthesis Mimics NA |
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Guanethidine |
Used for hypertension (high blood pressure) Depleted and replaces NA in vesicles and therefore in the nerve endings |
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Reuptake inhibitors |
DRIs = cocaine, amineptine NRIs = reboxetine SSRIs = Fluoxetine, citalopram, dapoxetine SNRIs = venlafaxine, duloxetine, tramadol |
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Cocaine |
Dopamine reuptake inhibitor |
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Amineptine |
Dopamine reuptake inhibitor A tricyclic antidepressant |
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Reboxetine |
Noradrenaline reuptake inhibitor Used for ADHD and depression |
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Fluoxetine |
Selective serotonin reuptake inhibitor Used for depression and sometimes OCD and bulimia |
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Dapoxetine |
Selective serotonin reuptake inhibitor Used for premature ejaculation |
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Verapamil |
Used to treat hypertension Cardiac calcium channel blocker |
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Ibuprofen |
Cyclo-oxygenase (enzyme) inhibitor to reduce inflammation |
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Phases of a drug trial |
Preclinical - non-human subjects, unrestricted dose with a graduate level researcher (PhD) Phase 0 - 10 subjects, sub-therapeutic dose, clinical researcher Phase 1- 20-100 subjects, sub therapeutic dose but ascending, clinical researcher Phase 2 - 100-300, therapeutic dose, clinical researcher Phase 3- 1000-2000, therapeutic dose, clinical researcher and personal physician Phase 4- anyone seeking treatment, therapeutic dose, personal physician |
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What happened to drug theralizumab? |
All 6 volunteers hospitalised in phase 1, 4 suffered multiple organ dysfunction. |
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What does bioavailability mean |
Proportion of the drug which has an active effect on the organism |
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What is latrogenicity |
The capacity to produce a disease from the side effects or inappropriate prescribing of drugs |
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What anti-malarial drug has neuropsychiatric side effects? |
Mefloquine or “Larium” |
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What is botulinum toxin used for |
Cosmetically to temporarily remove facial wrinkles Severe underarm sweating Cervical dystopia - neurological disorder that causes severe neck and shoulder muscle contraction Blepharospasm - uncontrollable blinking Strabismus - misaligned eyes |
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Why are concentration response curves useful? |
Useful to compare the potencies of different drugs that produce qualitatively similar responses |
