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(29 cards)
Sumatriptan (GPCR)
migranes
cetirizine (GPCR)
antihistamine
salbutamol (GPCR)
asthma
atenolol (GPCR)
hypertension
Asthma treatment
beta-agonists (salbutamol)
stimulate beta-2 adrenergic receptors that result in bronchodilation
GPCR antagonists
block overactive GPCRs for example from choleraetoxin (adds ADP ribose to G protein keeping it in an active state)
Malaria symptoms
Fever, vomiting, nausea, muscle pain, dry cough
Malaria species
Vivax, ovale, falciparum, malariae
Sulfonomides
Inhibit dihydropteroate synthase (which catalises formation of dihydropteroate)
Proguanil and pyrimethamine
Ihibits dihydrofolate reductate (catalises formation of tetrahydrofolic acid from dihydrofolate)
Quinine and chloriquine
Inhibits haem polymerase (formation of hemozoin)
Barbiturates
mass inhibition
used as anasthetics and epilepsy treatment
dangers: stop breathing
long term: tolerance, withdrawal symptoms
benzodizepines
Epilepsy and anixiety (diazepam)
potentiate effect og GABA
long term: tolerance, withdrawal symptoms
Ethanol biphasic (alcohol)
low dose: disinhibition (potentiates effect of GABA)
high dose: global inhibition (sedation, impaired function)
also stimulates dopamine release (euphoria)
NMDA receptor antagonist
Ketamine
Structure of local anasthetics
aromatic group-
ester/amide-
basic side chain (amine)
Drugs affecting neurotransmissiom
Haemocholinim (choline uptake inhibitor)
Triethylcholine (false transmitter)
Tyrosine kinase receptors
one agonist binds two TK
autophosphorylate eachother (SH2 protein is phosphorylated)
Conditions for schild to apply
B is a true competetive antagonist
A and B binding is mutually exclusive
Kb is constant
Same occupancy of A always gives the same response
system is at equilibrium
Chemical antagonism
antagonist binds to agonist not receptor (Heparin)
Functional antagonism
Antagonist is an agonist that produces the opposite effect (beta-adrenergic receptors to reduce asthma)
Pharmakokinetic antagonism
works to reduce the concentration of agonist (warfarin)
Indirect antagonism
works at a secondary downstream site (verapmil)
Vancomycin
Inhibition of Transglycosilation of peptidoglycan