Unit 1 Science Flashcards
What are adrenergic receptors?
Cell surface proteins that adrenaline and similar molecules bind to, resulting in cellular and physiological changes.
What differentiates receptor subtypes?
They have similarities in structure but differ in some amino acid residues, leading to different interactions with binding molecules.
What are ß-adrenergic receptor agonists?
Drugs that bind and activate ß-adrenergic receptors, such as salbutamol (ß2-adrenergic receptor agonist).
What are ß-adrenergic receptor antagonists?
Drugs that bind and prevent the action of ß-adrenergic receptors by agonists, such as propranolol (mainly ß1-adrenergic receptor antagonist).
Where is the ß1 adrenergic receptor found and what does it do?
Found in cells of the kidney and heart; causes heart muscle to contract.
Where is the ß2 adrenergic receptor found and what does it do?
Found in lung, vascular, and GI smooth muscle cells; causes smooth muscle to relax.
Where is the ß3 adrenergic receptor found?
Found in adipocytes (fat storing cells).
What are adrenaline and noradrenaline?
Endogenous hormones released from the adrenal gland at the top of the kidneys.
What are on-target side effects?
Effects on tissues where the intended target receptors are present.
What are off-target side effects?
Effects on different targets due to unselective binding, generally rare.
How does salbutamol act on the body?
Binds and activates ß2-adrenergic receptors on smooth muscle surrounding bronchi, causing relaxation and increased lung capacity.
What are the on-target side effects of salbutamol?
Increased blood glucose levels and rapid increase in lactic acid levels.
What are the off-target side effects of salbutamol?
Tremors, increased heartbeat, and palpitations due to action on ß1-adrenergic receptors.
What are beta-blockers?
ß-adrenergic receptor antagonists, such as propranolol.
What are non-selective beta blockers?
Beta-blockers with high affinity for both ß1 and ß2 receptors.
How does propranolol act as an antagonist for ß1-adrenergic receptors?
Competitively binds to the ß1-adrenergic receptor on cardiac myocytes, reducing heart rate and cardiac output.
What wider effects does propranolol have as an antagonist?
Reduces anxiety, prevents migraines, and reduces intraocular pressure.
What are the on-target side effects of propranolol?
Bronchoconstriction and dry eyes.
What is the typical agonist for serotoninergic 5-histamine receptors?
Histamine.
How do antihistamines work in allergic reactions?
They are receptor antagonists at H1 receptors, preventing histamine from binding and stopping physiological effects.
What side effect is caused by H1 antagonism?
Drowsiness and sleepiness due to effects in the CNS.
Why do some H1 antagonists cause drowsiness more than others?
Older drugs cross the blood-brain barrier more easily than newer antihistamines.
What properties increase the chance of drugs crossing the blood-brain barrier?
- High lipophilicity
- Small size and molecular weight
- Low hydrogen bonding potential
What is a common side effect of first-generation antihistamines?
Dry mouth or xerostomia.