4 Drugs
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What is an agonist?
• substance which initiates a physiological response when combined with a receptor (normally correcting something that has been lost)
What is a full agonist?
• bind to and activates a receptor, producing the maximum possible response that the tissue being targeted is capable of giving
What is a partial agonist?
• drugs that bind to and activate a given receptor, but have only partially produced the desired effect
What are the 2 types of agonists?
• partial and full agonists
How do agonists work?
• steroid hormone enters cell • binds to receptor protein • hormone receptor complex forms in nucleus • hormone receptor complex binds to specific gene sequences in DNA • genes are transcribed into mRNA which leaves nucleus • ribosomes translate mRNA into protein
What is the protein made by an agonist used for?
• protein made is essential to the cells function in some way
What does levothyroxine treat?
• hypothyroidism
Which hormone is deficient if dealing with hypothyroidism?
• Thyroxine (T4)
What type of drug is levothyroxine?
• agonist
Explain levothyroxine molecular basis of action
• levothyroxine binds to natural carrier protein in the blood • once it enters the cell it is metabolised into its active form L-triiodothyronine (T3) • T3 binds to thyroid receptor proteins in the cell nucleus • T3 receptor complex binds to specific areas of DNA and activates specific genes to make proteins
What are antagonists?
• occupies receptors but do not activate them, block receptor activation by agonists
What are the 2 types of antagonists?
• competitive and irreversible
What are competitive antagonists?
• slow down process by temporarily blocking a site or receptor
What are irreversible antagonists?
• stop a reaction permanently blocking a site or receptor
What type of drugs are beta blockers?
• competitive antagonists
Explain the molecular basis of action of beta blockers
• temporarily block receptor sites (beta adrenoceptors) for adrenaline and noradrenaline (hormonal neurotransmitters found in nervous system) • slows down but do not stop the impulse of the heart • slows down the rate and force of the heart muscle contraction is reduced, reducing blood pressure
What are beta blockers prescribed for?
• high blood pressure • angina • atrial fibrillation • heart failure
What is omeprazole prescribed for?
• Gastroesophageal reflux disease
What is omeprazole?
• proton pump inhibitor
Where are proton pumps found?
• stomach lining
What do proton pumps secrete?
• acid
What are the protons being pumped called?
• H+ ions
What type of drug is omeprazole?
• irreversible non competitive antagonist
Explain the molecular basis of action of omeprazole
• Proton pumps use active transport to move protons (H+) against a concentration gradient using ATP as energy into the lumen of the stomach • Omeprazole, a proton pump inhibitor, irreversibly binds to the ATP binding site- ATP cannot bind as protons move against the concentration gradient