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68 Cards in this Set

  • Front
  • Back
Norepinephrine's action on the CNS
Effects learning, memory, sleep/wake cycle, mood & anxiety

Affective disorders/ADD
Explain the effects of drug effects/side effects on the CNS (think about anti-depressants)
Over time there is an increase in the therapeutic effects

Over time the side effects tend to resolve
What is tolerance?
When taking a drug that effects the CNS over a period of time the body needs more to produce the same therapeutic effects.
What is physical dependence?
When stopping a drug suddenly causes a withdrawal syndrome.
What are some changes in drug absorption in the elderly?
Increased gastric pH
Decreased absorptive surface area
Deceased splanchnic (organ/intestinal) blood flow.
Decreased GI motility
Delayed gastric emptying
What are some PO absorption considerations in infants?
1. Prolonged/irregular gastric emptying (absorption is unpredictable, can be increased or delayed)
2. Infants have lower gastric pH, so more acid drugs are more readily absorbed and basic drug absorption can possibly be delayed
Pregnancy class A?
Remote risk of fetal harm

controlled studies show no harm in the first trimester, 2nd/3rd not tested.
Pregnancy class B?
Slightly more risk than A

Animal studies show NO risk & no studies have been done in women.

OR

Animal studies show risk but studies in women (1st tri) show NO risk. (2nd/3rd tri.not tested)
Pregnancy class C?
More risk than B

Animal studies may show risk & there have been no studies in women

OR

NO studies done in either animals or women

(this is the class most drugs are in because the classification system was put in place AFTER many of the drugs were put on the market)
Pregnancy class D
Proven fetal risk, but the benefits outweigh the risks. (asthma medications)
Pregnancy class X?
Proven fetal risk, benefits do not outweigh the risks (think accutane)
Changes in drug distribution in the elderly?
Increased body fat --> lipid soluble drugs are not distributed as efficiently because they are diffusing into the fat.

Decreased lean body mass + decreased H2O --> H2O soluble drugs have no where to diffuse so there is more free drug in the blood

Low albumin

Decreased CO
Consideration for drug distribution in neonates/infants?
Low albumin

BBB not fully developed
Changes in drug metabolism in the elderly?
Decreased metabolism --> increased half-life

Decreased first pass effects c PO medications
Ach life cycle?
1. Released in response to action potential

2. Binds to nicotinic/muscarinic receptors

3. Disassociates from receptor

4. Degradation almost immediately by ach-esterase

5. By product of degradation choline reabsorbed to make Ach again
Norepi. life cycle?
1. Released in response to action potiential

2. Binds to A1, A2, B1

3. disassociates

4. Re-uptake @ terminal

5. Stored in vesicles or degradation by monoaminoxidase (sp?)
Epi life cycle?
1. Synthesis in the adrenal medulla

2. Norepi is released and converts to epi

3. TRAVELS IN THE BLOOD to target organs

4. Disassociates

5. METABOLIZED by liver
B1 location & activation?
heart & kidneys

In the heart: Increases HR, increases contractility, and increased velocity @ the AV node.

In the kidneys: Renin--agiotensin-aldosterone cascade

BOTTOM LINE= INCREASED BP
What is the MAIN reason for geriatric non-compliance?
The belief that the drug is not needed and/or causes side effects
Other reasons for geriatric non-compliance?
Forgetfulness
Failure to understand instruction
$$
Complexity

Multiple: chronic disorders, Rx, prescribers

regimen changes
living alone
low literacy
hospital discharge
1. Selectivity of drugs that alter axonal conduction?
2. Why?
3. What type of drugs use axonal conduction?
1. LOW selectivity

2. Drugs that alter axonal conduction will affect ALL nerves it has access to

3. Local anesthetics
3 ways transmitters are removed from the synaptic gap?
1. Re-uptake by transport pump
2. Enzymatic degradation
3. Diffusion
7 main CNS neurotransmitters?
Ach
Epi
Norepi
Dopamine
Seritonin
Histamine
GABA
3 basic patterns of autonomic regulation?
1. balance/opposition (as seen in the heart)

2. complementary (erection-pns/ejaculation-sns)

3. innervation and regulation of only ONE of the autonomic systems (blood vessels)
5 step of synaptic transmission?
1. Transmitter synthesis
2 . " " storage
3. " " release
4. Receptor binding
5. Termination of transmission
3 main function of SNS?
1. Regulation of CVS
2. Thermoregulation
3. Fight-Flight
Ach action on the CNS?
excitatory
Ach is decreased with Alzheimer's

Has influence on: attention/memory/mood/aggression/sleep/muscle tone/thirst/deference
Epi action on the CNS?
low concentrations unlikely to play a role
Dopamine receptor function in SNS?
Dilate renal flood vessels

Increase cardiac contraction
Dopamine receptor function in CNS?
The most important receptor in the CNS

Generally INHIBITORY

hypothalamus, retina, limbic system, olfactory bulb, pituitary, cerebrum

D1 & D2 subtypes

Effects thoughts, emotions, movement, cognition/motivation
B2 receptor function?
Broncho-dilation
Relaxing of uterine muscle (you want that Baby 2 stay in there)

Increase Blood glucose

vasodilation, in the heart/lungs/skeletal muscle

VASODILATION...VASODILATION
A1 Receptor function?
"I'M CONSTRICTING"

Ejaculation (Alpha male, is #1 and spreads his seeds)

Contraction of bladder neck and prostate

Constriction of skin mucous membranes

Pupil dilation

VASOCONSTRICTION
A2 receptor function/location?
"STOP CONSTRICTING"

This receptor is located on the terminal end of the nerve itself NOT a target organ

INHIBITS A1

Helps reduce transmitter release where there is too much in the synaptic gap

VASODILATION
Epi acts on what receptors?
A1, A2, B1, B2
Norepi act on what receptors?
A1, A2, B1
Dopamine acts on what receptors?
A1. B1, & dopamine receptors
Primary peripheral nervous system receptors and their sub-types?
Cholinergic: nicotinic(n&m), muscarinic

Adrenergic: A1, A2, B1, B2, dopamine
What neurotransmitters do cholinergic receptors respond to?
Ach
What neurotransmitters do adrenergic receptors respond to?
Epi, norepi, dopamine
At what junctions is Ach the transmitter?
All preganglionic neurons

Postgang. neurons of the parasympathetic nervous system

Sweat glands (only place Ach is postgang in the SNS)

All skeletal muscle
Nicotinic N receptor function?
Release of epi from adrenal medulla
Nicotinic M receptor function?
muscle contraction
How selective is synaptic transmission? how?
HIGHLY SELECTIVE, synapses at different sites employ different transmitters
Finish the sentence:

The impact of a drug on a neuronally regulated process is dependent on...
the ability of the drug to influence receptor activity at the target cells
Three principal functions of the autonomic nervous system?
1. Regulation of the heart

2. Regulation of secretory glands

3. Regulation of smooth muscles
Serotonin functions in CNS?
Most is in the brain stem

regulation of sleep/pain/depression/mood/sex/aggression/appetite/pain control/temp regulation
Muscarinic 1-2-3 receptor function?
1. increased oral secretions, gastric acid and cognition

2. Decreased HR

3. Increased gladular secretions, pupil constriction, lens focus,
bronchoconstriction, increased GI motility, erection
Histamine's function in CNS?
Regulation of food/fluid intake, temperature, hormone release, sleep, allergic response mediation
Finish the sentence

Most nueropharmacologic agents act by___
altering synaptic transmission
Changes in drug excretion in the elderly?
Renal impairment/degeneration
What is the risk to a presomite when exposed to a teratogen?
If the dose is high enough (over lethal dose for presomite) = death

Usually if the dose is ANYTHING UNDER the lethal dose = generally no effects will be noticed
What is the risk to an embryo when exposed to a teratogen?
Gross malformations, because the limbs are forming
What is the risk to a fetus when exposed to a teratogen?
The brain is affected. Learning and behavioral problems may be noted
Neonate (1) and infant (2) absorption of IM medications?
1. Neonate: slow, erratic
2. Infants: faster than adults
Infant and neonate absorption of percutaneous medications?
Babies have thin skin, increased absorption
Drug metabolism in neonates/infants/children?
Neonates: metabolize SLOWER than adults

Infants: MUCH FASTER than adults

age 2: sharp decline

Puberty: gradual decline until another sharp decline at puberty when adult levels are reached.
Division of the peripheral nervous system
A. Somatic motor
B Autonomic...PNS & SNS
Renal excretion considerations in neonates/infants?
Slow excretion
At what age does drug absorption, distribution, and excretion reach adult levels?
ONE YEAR
At around what age does drug metabolism reach adult levels?
PUBERTY
Main ways drugs can effect receptor function and synaptic transmission
CAUSE receptor activation

BLOCK receptor activation

Enhance receptor activation by the natural transmitter at the site
Finish the sentence

The impact of a drug on a neuronally regulated process is _____
DEPENDENT on the ability of that drug to directly or indirectly influence receptor activity on target cells.
Lehne's definition of activation?
an effect on receptor function equivalent to that produced by the natural neurotransmitter at a particular synapse.
3 different effects drugs can have on transmitter synthesis?
1. Increased transmitter synthesis

2. Decreased transmitter synthesis

3. Cause the synthesis of transmitter molecules that are more effective than natural transmitters
drugs that interfere with transmitter storage will cause?
Receptor activation to decrease. Because there is less neurotransmitter available.
How can drugs effect transmitter release?
Either promote or inhibit transmitter release
3 ways drugs can effect receptor binding?
1. Bind to receptor and cause activation (agonist)

2. Bind to receptor and block activation (antagonist)

3. Enhance the natural transmitter activation
2 ways drugs can interfere termination of transmitter action?
1. Block reuptake (SSRI)

2.Inhibit transmitter degradation