NR 546 Psychopharmacology Week 2

Week 2

CYP450 Enzymes

A family of enzymes involved in the metabolism of various drugs and substances in the liver, playing a crucial role in pharmacokinetics and drug interactions.

Phase 1 metabolism: oxidation (most common), reduction, hydrolysis

3 possible outcomes: complete inactivation, multiple active metabolites, singular active metabolite

CYP 450 Inducers

VISA CK GQ

Valproate

Isoniazid

Sulfonamides

Amiodarone

Chloramphenicol

Ketoconazole

Grapefruit juice

Quinidine

CYP 450 Inhibitors

CRAP GPS

Carbamazepine

Rifampin

Alcohol

Phenytoin

Griseofulvin

Phenobarbital

Sulfonylureas

Dosing considerations when prescribing a CYP 450 Inducer

Prescribers should be aware that CYP 450 inducers can decrease the effectiveness of other medications by increasing their metabolism, potentially necessitating higher doses of those drugs to achieve the desired therapeutic effect.

Dosing considerations when prescribing a CYP 450 Inhibitor

Prescribers should recognize that CYP 450 inhibitors can increase the effectiveness of other medications by decreasing their metabolism, potentially leading to heightened effects or toxicity. May require decreased dosage.

Full agonists

are substances that fully activate a receptor, producing a maximum biological response.

Partial agonists

are substances that partially activate a receptor, resulting in a diminished biological response compared to full agonists.

Antagonists

are substances that bind to receptors but do not activate them, preventing other substances from eliciting a biological response.

Inverse agonists

are substances that bind to receptors and produce the opposite effect of agonists, leading to a decrease in the biological response below baseline function

Excitatory Neurotransmission

Neurotransmitters increase the likelihood of a neuron firing an action potential, facilitating communication between neurons.

Inhibitory Neurotransmission

Neurotransmitters decrease the likelihood of a neuron firing an action potential, inhibiting communication between neurons.

Reuptake Neurotransmission

Neurotransmitters are reabsorbed by the presynaptic neuron after transmitting a signal, thereby terminating the signal and recycling the neurotransmitters for future use.

Classic Neurotransmission

The process by which electrical impulses from neuron trigger neurotransmitter release from the presynaptic neuron, cross the synaptic cleft, and bind to receptors on the postsynaptic neuron. Postsynaptic neuron converts neurotransmitter input into an electrical signal, leading to excitatory or inhibitory effects.

Retrograde Neurotransmission

The mechanism by which postsynaptic neurons release neurotransmitters that travel back to bind to receptors on the presynaptic neuron, modulating neurotransmitter release and communication. Postsynaptic neuron “talks back”

Signal Transduction Neurotransmission

The process by which neurotransmitter binding to receptor sites on the postsynaptic neuron triggers a series of downstream biochemical events, leading to cellular responses such as changes in ion flow or gene expression.

Types of Signal Transduction Cascades

G-Protein-Linked: triggered by neurotransmitters, second messenger is chemical

Ion-Channel-Linked: triggered by neurotransmitters, second messenger can be an ion (i.e. calcium)

Hormone-Linked

Neurotrophin-linked