Pharmacology for Exam 2 Flashcards
What do non-competitive antagonists do?
They bind to a site on the receptor that keeps the channel closed but isn’t the same site as the NT. When the NT binds to its site on the receptor, it does not activate and the channel stays closed
What do MDMA and SSRI’s (Prozac, etc.) do? Agonist or antagonist?
Inhibit serotonin reuptake. Agonist
What does additional L-dopa do? Agonist or antagonist?
Increases dopamine production. Agonist
What do cocaine, amphetamines, and methylphenidate (Ritalin) do? Agonist or antagonist?
Inhibit dopamine reuptake. Agonist.
What two types of antagonists are there?
Competitive and non-competitive
What do cocaine, amphetamine, and Ritalin do?
Inhibit dopamine reuptake
What do SSRIs (Prozac) do?
Inhibit serotonin reuptake
What do migraine medications do? Agonist or antagonist?
Stimulate serotonin receptors. Agonist
What is an antagonist?
A drug that blocks or decreases the effect of a NT
What do MAO inhibitors do? Agonist or antagonist?
Interfere with the breakdown of monoamines including serotonin. Agonist
LOOK AT THE TWO CHARTS AT END OF NOTES
LOOK AT THE TWO CHARTS AT END OF NOTES
What do organophostaphates do?
They interfere with the enzyme AChE. Involved in enzyme degradation in the synapse
When the ligand fits perfectly with the receptor
High affinity
Any substance that alters the body or its functions
Drug
What does an increase in tryptophan from food do? Agonist or antagonist?
Increases serotonin production. Agonist
What do agonists do to receptors?
They activate receptors
Strength of association between ligand and receptor. How well it binds to the receptor
Affinity
What does apomorphine do? Agonist or antagonist?
Stimulates dopamine receptors. Agonist
Therapeutic index (wide vs narrow)
Wide is safe and narrow is risky. The line where the dose changes from mostly positive to mostly negative effects
What does nicotine do? Is it an agonist or antagonist?
Stimulates ACh receptors. Agonist
Amount of drug required to produce a certain response. Indicates power
Potency
Where do drugs act presynaptically?
NT production, NT storage, and NT release
What do drugs that treat the negative symptoms of schizophrenia do? Agonist or antagonist?
Block serotonin receptors. Antagonist
What may apomorphine be able to help treat?
Parkinson’s disease. Not currently approved for treatment, however.
Drugs that block the synaptic activity by occupying a binding site different from the NT on a receptor
Competitive or non-competitive antagonists
Property of a drug that determines its ability to produce its biological effect. How much response we are getting
Efficacy
Example of a drug affecting NT storage
Reserpine (used to treat mild to moderate hypertension) affecting storage of norepinephrine. Presynaptic
What is ED50?
The effective dose where you get 50% of the desired response
What do competitive antagonists do?
They bind to the site where a NT would bind and block it from binding with the receptor. The channel stays closed
How do drugs affect NT storage?
They interfere with the storage of a NT in vesicles within a neuron. Presynaptic
What are some things the body does with drugs?
Absorption, distribution, metabolism, and excretion
When the ligand fits with the receptor, but not perfectly
Medium affinity
What do drugs do to affect postsynaptic receptors?
Mimic the action of a NT at the site (agonist), block the synaptic activity by occupying a blinding site (competitive or non-competitive antagonist), and influence the activity of the receptor
Example of a drug affecting NT release
Botox. Presynaptic
What is the ceiling effect?
When the response to the drug levels out because the receptors are saturated
What does dietary choline do? Is it an agonist or antagonist?
Increases the production of ACh. Agonist
What is EC50?
The effective concentration where you get 50% of the desired response
What does curare do? Is it an agonist or antagonist?
It blocks ACh receptors. Antagonist
Drugs actions/effects and relationship in the removal from a synapse
Reuptake effects, enzymatic degradation, deactivation of NTs
What are the mechanisms for drug addiction?
By stage of NT life cycle, by interaction at specific NT synapse, prescribed medication, psychoactive drugs
How do agonists work?
They activate receptors and act as NTs. They block reuptake or enzymatic degradation
What do organophosphates do?Are they agonists or antagonists?
Block the action of acetylcholinesterase. Agonist
What does black widow venom do? Is it an agonist or antagonist?
Promotes ACh release. Agonist
How do drugs affect NT production?
They manipulate the synthesis of a NT to affect the amount available for release. Presynaptic
How do antagonists work?
They block receptors without activating them. They decrease the availability of NTs by reducing production of release
What the body does to drugs
Pharmacokinetics
When the ligand doesn’t really fit with the receptor
Low affinity
What does botulin toxin do? Is it an agonist or antagonist?
It blocks the release of ACh. Antagonist
How do drugs affect NT release?
They can modify the release of a NT in response to the arrival of an action potential. Presynaptic
Is it easier for drugs to create more or less of a NT?
Easier to make it less than more. Presynaptic
What drugs are involved in reuptake effects?
Cocaine, amphetamine, and Ritalin inhibit dopamine reuptake.
SSRIs (Prozac) inhibit serotonin reputake
What does MDMA (ecstasy) do? Agonist or antagonist?
Increases serotonin release. Agonist
What is an agonist?
A drug that mimics or enhances the effect of a NT
Drugs that mimic the action of a NT at their binding site on a receptor
Agonist
Where do drugs act postsynaptically?
They affect postsynaptic receptors
What do amphetamines do? Agonist or antagonist?
Increase the release of dopamine. Agonist
Relationship between concentrations of drug and biological effects. What drugs do to the body
Pharmacodynamics
What do most traditional schizophrenia medicines do? Agonist or antagonist?
Block dopamine receptors. Antagonist
What do antagonists do to receptors?
They block receptors without activating them
What do partial agonists do?
They mimic NTs but aren’t as good as a NT. Like opening a gate or channel but for not as long
Is it easier to make drugs influence glial cells or NTs?
NTs
What do full agonists do?
They mimic NTs and provide a response that is just as good as NTs
What does reserpine do? Agonist or antagonist?
Interferes with storage of dopamine and serotonin. Antagonist