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135 Cards in this Set

  • Front
  • Back

Drug

A chemical that in relatively small amounts effects physiology

Everything is a poison depending on its ____

Dose

Psychopharmacology

The study of how drugs effect the brain, interact with the brain, and how the body effects the drugs to interact with the brain

The neural tube becomes ___ and ___

The brain and spinal column

The neural tube "zips" together from ___ to ___ & ___

Middle, caudal and rostral

Cell proliferation

A process that increases the number of cells; most prominent in the 2nd trimester

Cell migration

A process in the development and maintenance of tissues during development, injury, and immune responses

Synaptogenesis

Formation of synapses between neurons in the NS. Occurs after growth cone reaches Target neuron

Organization of the brain determines its ____

Function

The 3 important parameters in brain organization

1. Density of neurons,


2. pattern of axon and dendrite branching, and


3. pattern of synaptic contacts

Parasympathetic preganglionic neurons use ____ as their main neurotransmitter

Acetylcholine

Preganglionic neurons are located in either the ___ or ____

Brain stem or spinal chord.

Postganglionic sympathetic neurons are ____ receptors

Adrenergic

Postganglionic parasympathetic neurons are _____

Cholinergic

Effects of norepinephrine and epinephrine vary among different target cells according to the types of ____ receptors they express

Adrenergic

Adrenergic receptors are ____ & ____

Alpha 1&2 and Beta 1&2

Two types of acetylcholine receptors

Muscarinic and nicotinic

Muscarinic and nicotinic receptors connect to ____ muscles and are responsible for voluntary movement

Striatum

Parasympathetic action = increased ____ activity

Acetylcholine

Which "gets your juices flowin'," cholinergic or anticholinergic?

Cholinergic. Anticholinergic = constipation

Pharmokinetics

How the body effects the drug

Pharmacodynamics

How the drug effects the body

ADMET

The absorption, distribution, metabolism, elimination, and time (how fast and how long a drug will appear at the Target)

Half life

Time to eliminate 1/2 of the drug in the body

Half life depends on both ____ and ____

Volume of distribution and clearance

T1/2 = ____

0.7 x volume of distribution ÷ clearance (0.7 is an approximate #)

The Blood Brain Barrier

A layer of brain epithelial cells that allow water, some gasses, selective transport molecules, and lipid-soluble molecules to pass into the brain

Aside from the BBB, ___ cells also serve as a barrier

Glial cells

___ and ___ are hydrophobic and pass the blood brain barrier

H and C

___ and ___ become polar and attract water due to hydrogen bonding and cannot pass the BBB

O and N

A ___ charge attracts more water and ____ lipid solubility

Positive, lowers

The change in charges in the BBB causes a change in ___ as well

pH

The ease at which a drug passes the ____ BBB impacts their psychoactive effectiveness

Blood Brain Barrier

____ is the primary energy source for the brain

d-glucose

Why does heroin feel more potent than morphine?

Heroin is more lipid soluble and passes the BBB 2-3x more effectively

Define Ligand

An Ion molecule that binds to a channel (i.e. a neurotransmitter, component of a drug)

Ligand gated ion channel

A group of ion channel proteins which open to allow ions (Na, K, Ca, etc) to pass through the membrane in response to the chemical messenger

The function of G-protein coupled receptors

They detect molecules outside the cell and activate cellular responses.

Define agonist

A chemical that binds to a receptor and activates it to produce a biological response

Define antagonist

A type of receptor ligand or drug that blocks a biological response by binding and blocking a receptor rather than activating it

Partial Agonist definition

Drugs that bind to and activate a receptor but only have partial efficacy in relation to a full agonist

Inverse agonist

A drug that binds to the same receptor as an agonist but induces a response opposite to the agonist.

Define partial inverse agonist

A drug that binds to the same receptors as an agonist, but induces the opposite effect of an agonist, in a lesser effect than a full inverse agonist

What % of people with depression receive treatment?

Less than 25%

Of those with depression that get treatment, ___ receive inadequate treatment

1/3

Of those with depression, less than ___ receive adequate treatment

10%

Risk of depression is ____ in women

Higher

Risk of depression is ___ in first degree relatives

Higher

Of those with depression, ___ will respond and recover

70%

Of those with depression, ___ of non-responders will respond to ECS therapy

20%

Of those with depression, ___ will not respond to any treatment

10%

Norepinephrine is synthesized from amino acid ____

L-tyrosine

Function of tyrosine hydroxylase

Responsible for catalyzing the conversion of the amino acid l-tyrosine for dopamine production

Function of DOPA decarboxylase

Responsible for the synthesis of dopamine from L-DOPA

Function of dopamine beta- hydroxylase

The only enzyme involved in the synthesis of small-molecule neurotransmitters, i.e. norepinephrine

Locus Coeruleus neurons project to the ____

Cerebral cortex

Antidepressants elevate ___ and ___ levels

Norepinephrine and serotonin

Antidepressants have a ___ week lag time for clinical improvement

2 week

Changes in receptor levels in depression appear to correlate with changes in ____

Mood

TCA stands for...

Tricyclic Antidepressants

TCA antimuscarinic effects include:

Memory dysfunction, dry mouth, increased eye pressure in glaucoma patients, constipation, decreased sweating, and blurred vision

TCA cardiovascular effects include:

Tachycardia, elevated norepinephrine, hypotension

TCA use should be limited in patients with:

Congestive heart failure, orthostatic hypotension, and advanced cardiovascular disease

TCA ____ vary widely, and may contribute to variability in effectiveness

Half life

Trazadone blocks ___ adrenergic receptors and ___ receptors

A1, H1

Trazadone side effects include:

Tachycardia, hypotension, may contribute to priapism, sedation

Bupropion (Wellbutrin, Zyban) is a ___ and ___ reuptake inhibitor

Dopamine and norepinephrine

Bupropion is as effective as ___ and ___ in treatment of depression

TCAs, SSRIs

Bupropion is ineffective in treatment of ___

Panic disorder

___ Reported to be effective in promoting smoking cessation

Wellbutrin

Adverse effects of bupropion (Wellbutrin, Zyban)

Insomnia, agitation, tremors, sweating, weight loss, seizures, diarrhea, sexual dysfunction

Dopamine activity can exacerbate psychosis in schizophrenia on this specific drug:

Bupropion (Wellbutrin, Zyban)

Bupropion is the generic name for:

Wellbutrin, Zyban

Due to their half lives, how many doses of SSRIs are needed per day?

Once

Long half life of norfluoxetine suggests a delay of ____ is required after stopping use before starting MAO inhibitor

1-3 month

Gastrointestinal side effects of SSRIs

Nausea, diarrhea, abdominal pain

CNS side effects of SSRIs

Anxiety, akathisia and agitation, insomnia

Endocrine effects in SSRIs

Sexual dysfunction in men

Symptoms of serotonergic syndrome

Excitement, diaphoresis, rigidity, hyperthermia, tachycardia, hypotension, coma, even death

____ have serious, even potentially fatal interaction with MAO inhibitors

SSRIs

Elderly metabolize ___ more slowly

SSRIs

Avoid use of this drug class during pregnancy

SSRIs

This class of drug has been known to activate mania

SSRIs

MAOI inhibits the activity of ___

Monoamine oxidase

There are ___ isoforms of MAO

2

MAOA metabolises ____ and ___

Norepinephrine and serotonin

MAOB metabolizes ____

Dopamine

Most MAO inhibitors are irreversible except ____

Moclobemide

Tyramine is a naturally occurring amine found in:

Cheeses, wines, certain foods (pickled fish, chocolate, coffee, yeast)

Tyramine is oxidized by ___

MAO

If tyramine is not metabolized, it can cause:

Hypertension, headache, fever, intracranial bleeding, death

Lithium may be less effective in treating patients with _____

Rapid cycling

In patients with rapid cycling, ___ and ___ may be more effective than lithium

Lamotrigine (Lamictal) and carbamazepine (tegretol)

____ may act by blocking inositol 1-phosphate in neurons with subsequent interruption of the 2nd messenger system

Lithium

____ reduces neuron responsiveness to muscarinic, alpha adrenergic, cholinergic, etc stimuli

Lithium

It is postulated that ___ stabilizes catecholamine receptors and may increase GABA activity

Lithium

Li+ has a ____ therapeutic index

Low

____ levels should be monitored every 2-3 days at first, then weekly for 4 weeks, then monthly, then quarterly

Lithium

____ treatment should be interrupted if patients exhibit fever, vomiting, or diarrhea

Lithium

___ treatment should be discontinued if patients will undergo surgery, have heart failure, or receive diuretics

Lithium

Lithium is safe for pregnancy after the ___ trimester

The 1st trimester

Gastrointestinal side effects of lithium

Nausea, vomiting, diarrhea

CNS side effects of lithium

General weakness, fine tremors

Cardiovascular side effects of lithium

EKG changes, arrhythmia

Lithium impacts on kidneys:

Polyurea due to reduced sodium reabsorption

Lithium impacts on endocrine system

Weight gain due to reduced thyroid function, diabetes

Dermatological impacts from lithium

Rash and acne, psoriasis, hair loss

Hematologic impacts of lithium

High white blood cell count

What are lithium toxicity levels?

Mild to moderate: 1.5-2.0mEq/L


Severe: 2.5-4.0mEq/L

What are symptoms of mild to moderate lithium toxicity?

Nausea, headache, vomiting, diarrhea, coarse tremor, ataxia, slurred speech, and confusion

Li overdose treatments:

Fluids and electrolyte replacement, forced diuresis with mannitol, urinary alkalinization, hemodialysis

Which anticonvulsants exhibit some utility in the treatment of bipolar disorder?

Depakote, Tegretol, and Lamictal

How does Tegretol work for bipolar?

It increases the inhibitory control of GABA, making it harder for neurons to fire.

Indications for Tegretol

manic phase of BD, rapid cycling in BD, treating depressive phase with antidepressants (to prevent mania or rapid cycling), to augment Antidepressants in tx-resistant depression

Mechanism of Tegretol

Blocks voltage dependent Na channels and inhibits paroxysmal depolarization shifts

Tegretol is not recommended in pregnancy due to risk of

Neural tube defects

Tegretol side effects are reduced by:

Slowly increasing dose

Gastrointestinal side effects of Tegretol

Nausea, vomiting, constipation, loss of appetite, diarrhea

CNS side effects of Tegretol

Sedation, dizziness, ataxia, confusion

You can use ___ either alone or with lithium to treat BD and schizoaffective

Depakote

Depakote is more effective than ___ in rapid cycling

Li

____ may be effective in treating depression compared to Tegretol or Li

Depakote

Pharmacodynamics of depakote

Decreased GABA metabolism with secondary increase to GABA concentration.

Dosing of Depakote

TID due to 8-10.5 hr half life

Pharmacokinetics of depakote

Metabolized by liver via beta oxidation, glucuronidation, and P450

What's the word on depakote and pregnancy?

Should not be used in pregnancy or breastfeeding, neural tube defects, fatal clotting abnormalities in infants

Side effects of depakote

Sedation, dizziness, nausea, vomiting, pancreatitis early in Tx

Pharmacodynamics of Lamictal

Unknown, but may effect sodium channels that modulate the release of excitatory transmitters

____ has a weak inhibitory effect on 5HT3 receptors

Lamictal

Most common side effects of Lamictal

Sedation, dizziness, diplopia, ataxia, decreased coordination, rash, steven-johnson syndrome, irritability, agitation, anxiety, depression, mania

Indications of (gabapentin) neurontin

Reports of effectiveness in mania may have been premature, although widely used in BD

Gabapentin is chemically related to ____, but does not act as ____ receptors. In fact, it may inhibits the reuptake of ___

GABA

Side effects of gabapentin

Somnolence, fatigue, ataxia, dizziness, weight gain, appetite change, easy bruising, joint pain, tremor, blurred vision, hostility

Mechanism of topamax

Blocks voltage-sensitive sodium channels and augments GABA activity while inhibiting NMDA-glutamate receptors

Adverse effects of Topamax

Dizziness, drowsiness, ataxia, constipation, nausea, vomiting, kidney stones