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Psychopharmacology Concepts
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Psychopharmacology Concepts
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What is Psychopharmacology?
Psychopharmacology is the study of the effects of drugs on the nervous system and behavior.
Define 'Drug' in the context of Psychopharmacology.
A drug is an exogenous chemical not necessary for normal cellular functioning that significantly alters the functions of certain cells of the body when taken in relatively low doses.
What are psychoactive drugs?
Psychoactive drugs are chemicals that alter the functions of cells in the nervous system.
What does 'Exogenous' mean?
Exogenous refers to being produced outside the body, which rules out chemical messengers produced by the body, such as neurotransmitters, neuromodulators, and hormones.
What are drug effects?
Drug effects are changes that can be observed in an individual's physiological processes and behavior.
What are sites of action in pharmacology?
Sites of action are the locations where drug molecules bind with molecules located on or in cells of the body to affect the biochemical processes of those cells.
What does pharmacokinetics include?
Pharmacokinetics includes the steps by which drugs are absorbed, distributed within the body, metabolized, and excreted.
What are the four main processes of pharmacokinetics?
The four main processes of pharmacokinetics are absorption, distribution, metabolization, and excretion.
How is a drug absorbed into the body?
A drug is absorbed into the body based on how it is administered.
What is the fastest route of drug administration?
The fastest route of drug administration is intravenous (IV) injection.
What is intraperitoneal (IP) injection?
Intraperitoneal (IP) injection involves injecting a drug through the abdominal wall into the peritoneal cavity, commonly used to administer drugs to lab animals.
Describe intramuscular (IM) injection.
Intramuscular (IM) injection is made directly into a large muscle, such as the upper arm or thigh, allowing absorption into the bloodstream through capillaries that supply the muscle.
What is subcutaneous (SC) injection?
Subcutaneous (SC) injection is when a drug is injected beneath the skin.
What are intracerebral and intracerebroventricular administrations?
Intracerebral administration involves injecting a very small amount of drug directly into the brain, while intracerebroventricular (ICV) administration involves injecting the drug into the cerebral ventricle for widespread distribution in the brain.
What is the primary drawback of IV injections?
The primary drawback of IV injections is the care and skill they require, as well as the fact that the entire dose reaches the bloodstream at once.
What is oral administration of drugs?
Oral administration is a method where drug molecules tend to reach sites of action slowly as they are absorbed into the blood through the digestive tract.
What is first-pass metabolism?
First-pass metabolism occurs when some drugs undergo metabolization by the liver after being absorbed, which reduces the number of active drug molecules available to produce an effect in the rest of the body.
What is sublingual administration?
Sublingual administration involves placing the drug underneath the tongue, where it is absorbed into the bloodstream through the capillaries that supply the mucous membrane lining the mouth.
What is the significance of lipid solubility in drug administration?
Lipid solubility is important because it determines the ability of fat-based molecules to pass through cell membranes; drugs that are lipid-soluble can more easily enter the brain.
What role does the liver play in drug metabolism?
The liver plays an especially active role in the enzymatic deactivation of drugs.
What is tolerance in drug administration?
Tolerance is when the effects of a drug diminish, requiring larger amounts of the drug for it to be as effective as it once was.
What are withdrawal symptoms?
Withdrawal symptoms are experienced by a person who has developed tolerance for a drug when they suddenly stop taking it, being primarily the opposite of the effects of the drug itself.
What is the therapeutic index?
The therapeutic index is a measure of a drug's margin of safety, obtained by administering varying doses of the drug to a group of lab animals or human volunteers.
What is the placebo effect?
The placebo effect is a response produced by an inactive substance when a person expects it to have a physiological or psychological effect.
What are synthetic drugs?
Synthetic drugs are completely artificial drugs that scientists produce.
What are antagonists and agonists?
Antagonists are drugs that block or inhibit the postsynaptic effects, while agonists are drugs that facilitate postsynaptic effects.
What is the order of synaptic events in neurotransmission?
The order of synaptic events includes neurotransmitter synthesis and storage in synaptic vesicles, vesicle travel to the presynaptic membrane, axon firing, calcium ion entry, neurotransmitter release into the synaptic cleft, binding to postsynaptic receptors, and reuptake or deactivation of neurotransmitters.
What are direct agonists and direct antagonists?
Direct agonists mimic the effects of a neurotransmitter and activate the receptor, while direct antagonists bind to the receptor but block it from being activated.
What is the difference between competitive binding and noncompetitive binding?
Competitive binding occurs when direct agonists and antagonists act on the neurotransmitter binding site, while noncompetitive binding occurs when molecules attach to alternative sites without competing with the neurotransmitter for the same binding site.
What are autoreceptors and their role in drug action?
Autoreceptors are a type of presynaptic receptor that regulates neurotransmitter synthesis and release; drugs that activate autoreceptors generally reduce synaptic communication.
What happens during vesicle transport in neurotransmission?
Vesicle transport involves filling synaptic vesicles with neurotransmitters using vesicle transporter molecules, which are distinct from terminal membrane transporters.
What is the role of receptors in drug action?
Receptors determine the effects of drugs depending on their location, the normal effects they mediate, and whether a drug activates or blocks their actions.
What role do terminal membrane transporters play in neurotransmitter reuptake?
Terminal membrane transporters are different from vesicle transporters and can be altered by drugs to block reuptake of neurotransmitters.
How do some drugs affect neurotransmitter action at transporters?
Some drug molecules attach to terminal membrane transporter molecules and inactivate them to block reuptake. Other drug molecules bind with enzymes that deactivate the neurotransmitter, preventing the enzymes from working.
What is the effect of drugs that block reuptake or enzymatic deactivation of neurotransmitters?
These drugs are considered agonists and prolong the presence of neurotransmitters in the synaptic cleft.
Which amino acid neurotransmitters are primarily involved in synaptic communication?
The two main amino acid neurotransmitters are glutamate (excitatory) and gamma-aminobutyric acid (GABA, inhibitory).
What is the role of glycine in the central nervous system (CNS)?
Glycine is a secondary inhibitory amino acid neurotransmitter found in the spinal cord and lower brain stem.
What is neurotransmitter modulation in the context of synaptic communication?
Most activity of local circuits of neurons involves the balance between excitatory and inhibitory effects of neurotransmitters.
What are the primary functions of glutamate in the CNS?
Glutamate is the main excitatory neurotransmitter, important for learning and memory.
How is glutamate synthesized?
Glutamate is synthesized from the precursor glutamine by the enzyme glutaminase.
What are the major types of glutamate receptors?
The major types of ionotropic glutamate receptors are NMDA, AMPA, and kainate receptors.
What is the role of NMDA receptors in synaptic transmission?
NMDA receptors play important roles in the cellular basis of learning and memory and allow sodium and calcium ions to enter the cell.
What is the significance of calcium ions in NMDA receptor function?
The entry of calcium ions serves as a second messenger that binds with and activates various enzymes in the cell.
What is the function of glycine in relation to NMDA receptors?
Glycine must attach to its binding site on NMDA receptors for the calcium channel to open.
What is the role of PCP (phencyclidine) in relation to NMDA receptors?
PCP binds with a site within the NMDA ion channel and serves as an indirect antagonist that prevents calcium ions from passing through.
How is glutamate removed from the synaptic cleft?
Glutamate is removed from the synapse by excitatory amino acid transporters and is broken down into glutamine by the enzyme glutamine synthase.
What is glutamate excitotoxicity?
Glutamate excitotoxicity can damage neurons by prolonged overexcitation, believed to be involved in brain damage from stroke and amyotrophic lateral sclerosis.
What is GABA and what is its primary role in the brain?
GABA (gamma-aminobutyric acid) is an inhibitory neurotransmitter that plays a crucial role in stabilizing neural interconnections to prevent seizures.
How is GABA synthesized?
GABA is produced from the precursor glutamic acid by the enzyme glutamic acid decarboxylase (GAD).
What is the primary receptor type for GABA?
GABAA receptors are the primary ionotropic receptors that control chloride channels.
What drugs serve as agonists and antagonists of GABAA receptors?
Muscimol is an agonist for GABAA receptors, while bicuculline blocks GABA binding, serving as an antagonist.
What is the role of benzodiazepines in relation to GABAA receptors?
Benzodiazepines, such as diazepam and alprazolam, bind to a site on GABAA receptors to produce anxiolytic and muscle relaxant effects.
What is the mechanism of action for barbiturates concerning GABAA receptors?
Barbiturates bind to GABAA receptors and enhance the inhibitory effects of GABA.
How is GABA deactivated in the synaptic cleft?
GABA is removed from the synapse by GABA transporters and is deactivated by the enzyme GABA aminotransferase.
What is acetylcholine (ACh) and its functions in the nervous system?
ACh is a neurotransmitter that functions in both the CNS and PNS, controlling muscle contractions in the PNS and facilitating learning in the CNS.
What enzymes are involved in the synthesis of ACh?
Choline acetyltransferase (ChAT) is required to produce ACh from its precursors, choline and acetylcoenzyme.
What is the effect of botulinum toxin on ACh release?
Botulinum toxin prevents the release of ACh, causing paralysis.
What are the types of receptors for acetylcholine?
ACh has ionotropic nicotinic receptors and metabotropic muscarinic receptors.
How does AChE function in neurotransmitter deactivation?
Acetylcholinesterase (AChE) breaks down ACh into its precursors, allowing for recycling.
What is the role of dopamine in the brain?
Dopamine is involved in important functions like movement, attention, learning, and reinforcing effects of drugs.
What are the main pathways of dopamine production?
The three main pathways are the nigrostriatal system, mesolimbic system, and mesocortical system.
What causes Parkinson's disease in relation to dopamine?
Degeneration of dopaminergic neurons connecting the substantia nigra with the caudate nucleus causes movement disorders characteristic of Parkinson's disease.
What is the precursor for dopamine and norepinephrine?
Tyrosine is the essential amino acid precursor for both dopamine and norepinephrine.
What is the effect of the drug chlorpromazine on dopamine receptors?
Chlorpromazine blocks D2 receptors and alleviates symptoms such as hallucinations in schizophrenia.
How are dopamine transporters involved in neurotransmitter reuptake?
Dopamine transporters are responsible for removing dopamine from the synapse.
What is the action of amphetamine and methamphetamine on dopamine release?
Amphetamine and methamphetamine cause the release of dopamine and norepinephrine by making the transporters for these neurotransmitters less effective.
What role do neurotransmitters play in the brain?
Neurotransmitters facilitate communication between neurons and are involved in various brain functions.
What is the effect of cocaine and methylphenidate on neurotransmitters?
Cocaine and methylphenidate block dopamine reuptake.
How is catecholamine deactivation regulated?
Catecholamine deactivation is regulated by an enzyme called monoamine oxidase (MAO).
Where is monoamine oxidase (MAO) found?
MAO is found within monoaminergic terminal buttons where it deactivates excess neurotransmitters.
What is deprenyl, and what is its function?
Deprenyl is a drug that inhibits the particular form of monoamine oxidase (MAO-B) and serves as a dopamine agonist used to treat symptoms of Parkinson's disease.
Where are noradrenergic neurons located?
Cell bodies of noradrenergic neurons are located in 7 regions of the pons and medulla and one region in the thalamus.
What is the locus coeruleus?
The locus coeruleus is a nucleus located in the dorsal pons where the cell bodies of the most important noradrenergic system begin.
How is norepinephrine synthesized?
Norepinephrine is synthesized from dopamine, and the enzyme dopamine beta-hydroxylase facilitates this process.
What is the function of the drug AMPT?
AMPT prevents the conversion of tyrosine to L-DOPA, blocking the production of norepinephrine as well as dopamine.
How are most classical neurotransmitters synthesized?
Most classical neurotransmitters are synthesized in the cytoplasm of the terminal button and then stored in newly formed synaptic vesicles.
What is the role of 2ABP in neurotransmitter synthesis?
Furasic acid inhibits the activity of dopamine beta-hydroxylase and blocks norepinephrine production without affecting dopamine production.
What types of adrenergic receptors exist?
There are four types of adrenergic receptors: Alpha 1, Alpha 2, Beta 1, and Beta 2.
What is the significance of idazoxan in research?
Idazoxan is a research drug that blocks alpha 2 autoreceptors and acts as an agonist used to study the actions of the norepinephrine system.
What is the norepinephrine transporter?
The norepinephrine transporter is responsible for removing excess norepinephrine from the synapse.
What is the role of MAO-A in norepinephrine deactivation?
Monoamine oxidase MAO-A deactivates norepinephrine.
What is moclobemide?
Moclobemide specifically blocks MAO-A and serves as an noradrenergic agonist.
What are the primary functions of serotonin?
Serotonin is involved in mood regulation, pain regulation, control of eating, sleep, arousal, and dreaming.
Where are serotonergic neuron cell bodies located?
Cell bodies of serotonergic neurons are found in nine clusters located in the raphe nuclei of the midbrain, pons, and medulla.
What is the precursor for serotonin?
The precursor for serotonin is tryptophan.
What does tryptophan hydroxylase do?
Tryptophan hydroxylase acts on tryptophan to produce 5-HTP (5-hydroxytryptophan).
What is the function of 5-HTP decarboxylase?
5-HTP decarboxylase converts 5-HTP to 5-HT (serotonin).
What is the role of PCPA?
PCPA (p-chlorophenylalanine) is a drug that blocks the activity of tryptophan hydroxylase, serving as a serotonergic antagonist.
How many types of serotonin receptors are there?
There are at least nine different types of serotonin receptors.
What is the role of 5-HT1A receptors?
5-HT1A receptors serve as autoreceptors in the membrane of dendrites and soma in the dorsal and median raphe nuclei.
What is ondansetron?
Ondansetron is a 5-HT3 antagonist useful in reducing nausea side effects of chemotherapy and radiation.
What is buspirone (BuSpar)?
Buspirone (BuSpar) is a partial 5-HT1A agonist that treats symptoms of anxiety and depression.
What is the effect of LSD on serotonin receptors?
LSD (lysergic acid diethylamide) is a direct agonist for postsynaptic 5-HT2A receptors in the forebrain that produces distortions of visual perception.
What is the function of the serotonin transporter?
The serotonin transporter removes 5-HT from the synapse.
What is fluoxetine (Prozac)?
Fluoxetine (Prozac) is a drug used to treat depression, some forms of anxiety disorder, and obsessive-compulsive disorder.
What is the role of fenfluramine?
Fenfluramine causes the release of serotonin as well as inhibits its reuptake.
What does MDMA do?
MDMA (methylenedioxymethamphetamine, or ecstasy) binds with norepinephrine and 5-HT transporters and causes them to run backwards, releasing neurotransmitters and inhibiting their reuptake.
Where are histaminergic neurons located?
Histaminergic neurons are found in the tuberomammillary nucleus located in the posterior hypothalamus.
What is the role of histamine in the brain?
Histamine plays an important role in wakefulness.
How is histamine produced?
Histamine is produced from the amino acid precursor histidine by the action of the enzyme histidine decarboxylase.
What are the receptors in the CNS that histamine interacts with?
The CNS contains H1-4 receptors.
What is the effect of diphenhydramine?
Diphenhydramine is found in many over-the-counter sleep aids and allergy medicines and crosses the blood-brain barrier, producing drowsiness.
What are peptides in the context of neurotransmitters?
Peptides consist of two or more amino acids linked together by peptide bonds.
How are peptides produced and released?
Peptides are synthesized in the soma and transported to the terminal button, where they are released along with classical neurotransmitters.
What are endogenous opioids?
Endogenous opioids are a family of peptides that reduce pain, including substances like opium, morphine, heroin, and oxycodone.
What are the three different types of opioid receptors?
The three different types of opioid receptors are Mu, Delta, and Kappa.
What is naloxone?
Naloxone is used to clinically reverse an opioid overdose and can save lives.
What are endocannabinoids?
Endocannabinoids are natural ligands for the receptors responsible for the effects of THC.
What does THC do?
THC (tetrahydrocannabinol), the active ingredient in marijuana, produces analgesia and sedation, stimulates appetite, reduces nausea, and alters perception.
What is anandamide?
Anandamide is a lipid-like substance discovered to be the first natural ligand for the THC receptor.
How do lipid neurotransmitters function?
Lipid neurotransmitters appear to be synthesized on demand and are produced and released as needed, rather than being stored in synaptic vesicles.
What are the CB1 and CB2 receptors?
CB1 and CB2 are metabotropic receptors that interact with endocannabinoids.
What is the effect of rimonabant?
Rimonabant is a drug that blocks the CB1 receptors.
What happens when CB1 receptors are activated?
When CB1 receptors are activated, they open potassium channels in the terminal buttons, shortening the duration of the action potential and decreasing the amount of neurotransmitter released.
What is the role of FAAH?
FAAH (fatty acid amide hydrolase) is an enzyme that deactivates anandamide.
What are anandamide transporters?
Anandamide transporters are molecules that transport anandamide back into the neurons.
What is MAFP?
MAFP is a drug that inhibits FAAH, acting as a cannabinoid agonist.
What does AM1172 do?
AM1172 is a drug that inhibits cannabinoid reuptake.
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Explore key concepts in psychopharmacology, including drug effects and psychoactive substances.
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