Mid Semester Question Bank Flashcards
What factor does not contribute to inter-individual variation?
Blood type
What is a peptide inhibitor?
A substrate that binds to the SH2 domain of proteins
–> Prevents dimerization with the intra-cellular part of the receptor
Kinase-linked receptors…
Have a very slow release
Name all types of antagonists:
- Competitive
- Non-competitive
- Functional
The sequence of nuclear receptors:
- Drug binds to receptor
- Receptor homo-dimerizes
- Receptor activated gene transcription
- Protein is made
What determines the occupation of receptors during drug-receptor binding?
Affinity
What is a partial agonist?
A drug that produces a lowered maximal effect
How do receptors act as drug targets?
A drug can bind to a plasma membrane receptor to trigger signalling
What is potency?
- The measure of affinity for the drug to receptor
- The x-shift on a dose-response curve
What is true about side effects and adverse effects of a drug?
Side effects are experienced within the therapeutic range.
Adverse effects are experienced beyond the therapeutic range
What does an agonist do?
An agonist binds to the active site
Through which routes are drugs eliminated?
Expired air
Feces and urine
How do dietary constituents inhibit metabolism?
Some molecules like cyclosporin –> hydroxyclyclosporin inhibit metabolism of other drugs
What governs the absorption in the intestine?
Weak acids and weak bases are well absorbed
How are drugs absorbed into the body?
- Oral
- Rectal
- Percutaneous
- Intramuscular
- Intrathecal
- Inhalation
What is the correct process for metabolism of aspirin?
Aspirin is hydrolized to salicylate and acetic acid by esterase in tissue and blood
Phase 2 reactions involve:
- A cofactor donor group
- Transferases transfer water soluble groups to a receptor
K1 and K2 values are determined by…
- Blood flow
- Drug lipophilicity
- Plasma
- Tissue barriers
Absorbtion via the GI is dependant on:
- Concentration gradient
- Lipophilicity
- Blood flow to site of absorption
- Drug formulation
How does induction effect paracetamol?
Increased CYP metabolite –> toxicity
Principle points for protein binding:
- Only unbound drugs can diffuse into peripheral tissue
- Albumin is an important co-factor in drug binding
- Plasma protein binding can be saturable for some drugs
Induction of CYP proteins leads to:
Increased metabolism of substrate and lower plasma drug levels
Oral bioavaliability:
The fraction of an oral dose that reaches systemic circulation
What determines the diffusion of drugs into peripheral tissue?
- Drug size
- Degree of ionization
- Lipid solubility
What are the two different ACh receptors found in the parasympathetic division?
- Nicotinic
- Muscarinic
Which neurotransmitter is released by preganglionic and postganglionic fibers in the parasympathetic division of the ANS?
Acetylcholine
What are the two different ACh receptors found on postsynaptic membranes in the parasympathetic division?
Nicotinic and musacarinic
Side effects of Mirtazapine:
Dry mouth
Weight gain
Sedation
Dopamine is degraded by MAO. T/F
True
MOA:
-> increased NA (and 5-HT)
levels in synaptic cleft due to
uptake inhibition
Direct acting agonists or antagonists can act at postsynaptic receptors. T/F
True
Indirect acting agonists release neurotransmitters from presynaptic nerve terminals to
produce a sympathomimetic effect, such as _____
amphetamines
Specific drugs can inhibit the Ca2+-dependent release of noradrenaline, thus having a
_____ effect
sympatholytic
Drugs such as reserpine cause the…
destruction of storage granules, and as a result,
depletion of the synaptic terminal of noradrenaline which is also a sympatholytic action.
Inhibition of the membrane uptake of catecholamines by drugs such as cocaine and
tricyclic antidepressants produce…
a sympathomimetic effect
Inhibition of monoamine oxidase by drugs such as some ____
antidepressants.
The IP3 and DAG pathway leads to:
Contraction
The cAMP pathway leads to:
Relaxation
What type of medication is given to decrease
sympathetic stimulation, resulting in decreased
heart rate?
Beta-blockers
Beta-blockers act by:
lowering your blood pressure by blocking the effect of hormones called adrenaline and noradrenaline
What are the functions of the ANS
Regulation of:
- Body temp
- Cardiovascular activity
- Digestive functions
The 2 main colinergic receptors:
Nicotinic an muscarinic
What agonizes the nicotinic receptors?
Acetylcholine and nicotine
What symptoms would you expect if you ingested a muscarinic agonist?
Salvation Lacrimation Urination Defecation Gastro Emisis Bronchospasm Bronchodilation Bradycardia
Acetylcholinesterase inhibitors can:
Treat glucoma
Cause diarrhea
Side effects of nicotine:
Mydriasis Tachycardia Weakness Hyperthermia Fasciculation
Beta1-receptor activation leads to:
Contraction of the heart
Sympathomimetic drugs act to:
Agonise at a1, b1 and b2 receptors
Sympatholytic drugs act to:
Agonise at a1, b1 and b2 receptors
and;
antagonise at alpha2 receptors
Indirect sympathomimetic drugs:
- NA uptake inhibitors
- MAO-inhibitors
- Amphetamine,
- Ephedrine
Beta-blockers can be used to treat:
Hypertension
What is the adrenergic effect at target organs?
Vasodilation in skeletal muscle
Nicotine causes:
Mydriasis
Hyperthermia
Fasiculations
Weakness
Nicotine does not cause constipation. T/F
True