keep forgetting !! Flashcards
what effect can pharmacokinetic antagonists have - give example
Some antibiotics increase the metabolism of drugs like warfarin, reducing its effective concentration in the blood steam
what is physiological antagonism, give example of this
When two or more drugs interact with opposing actions in the body or act through separate cells/difference transduction systems
eg. Noradrenaline raises arterial blood pressure by acting on the heart and peripheral blood vessels while histamine acts to reduce arterial blood pressure by causing vasodilation
give the action of Non-competitive antagonists , give an example
do not compete with the agonist but block some step in theprocess between the receptor and the response
e.g. Dihydropyridines bind to an block Ca 2+ channels rather than the receptor itself which is activated by noradrenaline
what are prostoglandins
lipids made ad the site of infection of tissue damage
control - inflammation, blood flow, clotting, uterus contraction
what can inhibit the Na+/K+ pump
cardiac glyscosides - oaubain and digoxin
what is the metformin transporter
OCT 1
what is the paracetamol intermediate
NAPQ1 its toxic
what is cyclosporin and what is its action
immunosuppressant for rheumatoid arthritis,Crohn’s disease, in organ transplants
bidns to cycloophillin in the cell, blocks action of calcineurin, dephospho rylation of NF kappa Beta so no transcription of cytokines
3 things that can be done to change the open probability of a transporter
HC03
pH change
Gprotien
anion concentration in the cell
65 IC
0 EC
what family is the Ca2+ pump in
the Ptype ATPase family
when activated what will PLC cause
PIP2 to split into IP3 and DAG
what can activate Ryanodine receptors
ryanodine, cADP ribose and caffeine
what inhibits AE3
DIDS
how many TM domains does AE have
14 > 8 is important in transport
How many TM domains does NHE1 have
12
what inhibits NHE1
ammiloride /EIPA
what activates PKC
calcium
what activates PKA
ATP
example of and antioxidant
asorbic acid
example of a free radical scavenger
ethanol
example of a chemical antagonist
dimercaprol
how to limit desensitisation
add antagonist
2 adverse reactions you can have to biopharmaceuicals
- exaggerated pharm - hgiher specificity than planned
2. Antidrug antibody reaction - accelerated clearance or exposure prolonged
what is the partition coefficient
measure of the lipophilicity of a drug and an indication of its ability to cross the cell membrane
what does a high partition coefficent show
efficient at entering the lipid compartment - usually non polar
Are more rapidly filtered by kidneys though
want a high PC for CNS drugs
pH in stomach, plasma and kidneys/urine
stomach - 2.5.
plasma 7.1
kidneys/urine 8
2 things that can and 2 that cannot cross the BBB
can - Ethanol and caffeine
Cant - chemotherapy drugs, antibiotics
3 types of Prostanoids
prostoglandis, thromboxanes prostocyclins
what do thromboxanes do and example
mediate vasoconstriction and clot formation eg. (TXA2)
role of prosotocyclins
inhibit platlet aggregation and vasodalation
COX 1 role and location
in kidney and colon, on all the time, produce prostaglandins involved in platelet aggregation and mucus secretion
asprin role, where absorbed and what can it treat
rapidly absorbed in the ileum
prevents COX 1 working so stomach ulceration
can treat - alzheimers, colon caner and thrombosis
what is rheumatoid arthritis and risk factors (2)
inflammation of the synovial joint
genetics and smoking
activation of TH1 cells results in
- activates macrophages
- they secrete cytokines
- recruit cells that erode cartilage and bone (fibroblasts and osteoblasts )
3 types of DMARDs and there action
methotrexate - folic acid antagonist
sulfasalazine
drugs with metal ions - free radical scavengers
mast cells role and role in late stage asthma
release granules to fight parasitic infections
in late stage asthma - mast cell activation causes inflammation, cytokines cause leukocytes infiltration
TH2 cell activity
make IgE antibodies
