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(MUL) Pharmacology > (Ch 18) CNS Introduction > Flashcards

(Ch 18) CNS Introduction Flashcards

1
Q

Name the main CNS neurotransmitters

(6)

A
  1. Noradrenaline
  2. Dopamine
  3. 5-HT
  4. Acetylcholine (Ach)
  5. GABA (Gamma-aminobutyric Acid)
  6. Glycine
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2
Q

Noradrenaline (Norepinephrine)

Recall 6 points

A

Noradrenergic transmission is important in control of mood (functional deficiency resulting depression) controlling wakefulness, and alertness

  1. Catecholamine that is the neurotransmitter of most sympathetic postganglionic neurons and also of certain tracts in the central nervous system.
  2. Neurohormone stored in the chromaffin granules of the adrenal medulla and released inresponse to sympathetic stimulation, primarily in response to hypotension.
  3. It produces vasoconstriction, an increase in heartrate, and elevation of blood pressure.
  4. It is administered intravenously in the form of the bitartrate salt as a vasopressor to restore blood pressure in certain cases of acute hypotension and to improve cardiac function during decompensation associated with congestive heart failure or cardiovascular surgery.
  5. Called also noradrenaline
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3
Q

NS consists of

A
  1. Brain
  2. Spinal Cord
  3. Nerves
  4. Ganglia

Collectively receive stimuli and transmit information

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4
Q

Drug Ex: for Norepinephrine

A

norepinephrine bitartrate

Levophed, Noradrenaline (UK)

  • Pharmacologic class:* Sympathomimetic
  • Therapeutic class*: Alpha- and beta-adrenergic agonist, cardiac stimulant, vasopressor

Pregnancy risk category C

FDA Box Warning

If extravasation occurs (Extravasation is the leakage of a fluid out of its container into the surrounding area, especially blood or blood cells from vessels) infiltrate area promptly with 10 to 15 ml of saline solution containing 5 to 10 mg phentolamine toprevent sloughing and necrosis. Use syringe with fine hypodermic needle, and infiltrate solution liberally throughout area.Give phentolamine as soon as possible; its sympathetic blockade causes immediate local hyperemic changes if area is infiltrated within 12 hours.

Action

Stimulates beta1 and alpha1 receptors in sympathetic nervous system, causing vasoconstriction, increased bloodpressure, enhanced contractility, and decreased heart rate

Availability

Injection: 1 mg/ml

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5
Q

What types of receptors are most commonly found in the CNS?

A
  1. Ion-gated receptors (Na+, K+, Cl–, Ca2–)
  2. Ligand-gated receptors (Ligand-gated ion channels ( LICs, LGIC ), also commonly referred to as ionotropic receptors, are a group of transmembrane ion-channel proteins which open to allow ions such as Na +, K +, Ca 2+, and/or Cl − to pass through the membrane in response to the binding of a chemical messenger (i.e. a ligand ), such as a neurotransmitter)
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6
Q

Define

Dopamine

A

1. Dopamine is important in motor control (Parkinsonism is due to dopamine deficiency)

  1. Has behavioural effects (excessive dopamine activity is implicated in schizophrenia)
  2. Important in hormone release (prolactin, GH) and dopamine in chemoreceptor trigor zone causes nausea and vomiting.
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7
Q

Define Seratonin

Seratonin also known as _____?

A
  1. Physiological functions associated with 5-HT pathways include; feeding behaviour, behavioural response (hallucinatory behaviour), control of mood and emotion, control of body temperature and vomiting.
  2. 5-HT
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8
Q

Acetylcholine has effects on what ?

A
  1. Acetylcholine (Ach). Ach has effects on arousal, on learning, and on short-term memory.
  2. Dementia and parkinsonism are associated with abnormalities in cholinergic pathways.
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9
Q

Define Acetylcholine

A
    1. Acetylcholine*, an ester of choline and acetic acid that serves as a transmitter substance of nerve impulses within the central and peripheral nervous systems.
      1. Acetylcholine is the chief neurotransmitter of the parasympathetic nervous system, the part of the autonomic nervous system (a branch of the peripheral nervous system) that contracts smooth muscles, dilates blood vessels, increases bodily secretions, and slows heart rate.
      2. Acetylcholine can stimulate a response or block a response and thus can have excitatory or inhibitory effects.
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10
Q

Define GABA and what does it stand for?

A
  1. GABA is an Chief inhibitory neurotransmitter in CNS.
  2. Gamma-amino butyric acid
  3. Its principal role is reducing neuronal excitability throughout the nervous system.
  4. This means you are protected from nerve impulses. This neurotransmitter cools the brain.
  5. it helps to increase alpha wave production. This is related to the feeling of relaxation we have in brains.
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11
Q

Glycine Neurotransmitter

A
  1. Glycine. is an inhibitory neurotransmitter, acts on GABA like receptor in the spinal cord.
  2. Glycine is an inhibitory neurotransmitter in the central nervous system, especially in the spinal cord, brainstem, and retina.
  3. When glycine receptors are activated, chloride enters the neuron via ionotropic receptors, causing an inhibitory postsynaptic potential (IPSP).
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12
Q

What are the primary functions of a neurotransmitter?

A

To bind a receptor and subsequently either excite or inhibit the postsynaptic neuron

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13
Q

What are EPSPs?

A

Excitatory postsynaptic potentials— initiated when an excitatory neurotransmitter activates Na+ or Ca2+ channels

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14
Q

CNS consist of

A

The central nervous system consists of the brain and spinal cord.

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15
Q

Peripheral nervous system (PNS):

name 2 divisions:

A
  1. Somatic nervous system (SNS): acts on skeletal muscles to produce voluntary movement and respiration.
  2. Autonomic nervous system (ANS): known as the visceral system, is responsible for involuntary movement and controls the heart, respiratory system, gastrointestinal system, and endocrine system (glands).
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16
Q

Autonomic Nervous System is organized in 2 divisions:

A

1. Sympathetic nervous systems:

2. Parasympathetic nervous systems:

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17
Q

Define Sympathetic nervous systems:

A

1. Sympathetic nervous systems: called the adrenergic system and uses the norepinephrine neurotransmitter to send information. It is also referred to as the thoracolumbar division of the autonomic nervous system.

The sympathetic system excites organs (increases heart rate).

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18
Q

Defien Parasympathetic nervous systems:

A

2. Parasympathetic nervous systems: The parasympathetic system, called the cholinergic system, uses the acetylcholine neurotransmitter to transmit information. It is also known as the craniosacral division of the autonomic nervous system.

The parasympathetic system inhibits the organs (decreases heart rate).

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19
Q

Give 5 examples of excitatory neurotransmitters.

A
  1. Norepinephrine
  2. Dopamine
  3. Acetylcholine
  4. Glutamate
  5. Aspartate
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20
Q

What are IPSPs?

A
  1. Inhibitory postsynaptic potentials— initiated when an inhibitory neurotransmitter opens Cl–, channels and the cell membrane becomes hyperpolarized.
  2. IPSPs make it more difficult for the neuron to become activated.
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21
Q

Give 2 examples of inhibitory Neurotransmitters

A
  1. Glycine
  2. GABA

Are considered what type of Neurotransmitters?

22
Q

In general, how do drugs affecting the CNS work?

A
  1. Most drugs will affect the production, storage, release, reuptake, or metabolism of a neurotransmitter.
  2. Other agents may directly affect the postsynaptic receptor.
23
Q

What are the major differences between the autonomic nervous system of (PNS) and the central nervous system?

A

There are 3 major differences:

  1. The number of neurotransmitters is greater in the CNS.
  2. The number of synapses is greater in the CNS.
  3. The CNS, unlike the autonomic nervous system, has a large array of inhibitory neurons that serve to modulate action.
24
Q

Pathologic Pathways extending from _____ to ____.

These pathways contain two types of nerve fibers that are connected together by a ______.

Name 2 type of Nerve Fibers:

A
  1. Neurologic pathways extend from the spinal cord to parts of the body.
  2. Ganglion

a. Preganglionic fibers: The preganglionic nerve fiber carries messages from the central nervous system to the ganglion.

A preganglionic nerve fiber is long—from the spinal cord to the ganglion.

b. Postganglionic fibers: The postganglionic nerve fiber transmits messages from the ganglion to specific tissues and organs.

A postganglionic nerve fiber is relatively short—from the ganglion to the cells of the body.

25
Q

Neurologic pathways in the sympathetic nervous system originate from?

A

Neurologic pathways in the sympathetic nervous system originate from the thoracic (T1 to T12) and the upper lumbar segments (L1 and L2) of the spinal cord.

26
Q

Neurologic pathways in the parasympathetic nervous system originate from?

A

Neurologic pathways in the parasympathetic nervous system originate from cranial nerves III, VII, IX, and X, from the brainstem, and the sacral segments S2, S3, and S4 from the spinal cord.

This is why the parasympathetic nervous system is also known as the craniosacral division of the autonomic nervous system.

27
Q

What are 4 major groups of medication that stimulate the CNS

A
  1. Amphetamines
  2. Caffeine
  3. Analeptics
  4. Anorexiants
28
Q

Amphetamines:

A

Amphetamines stimulate the cerebral cortex of the brain.

Amphetamines are also taken to decrease weight and increase energy, enabling performing work quickly without rest.

29
Q

Caffeine:

& found in what other (4) medications

A

Caffeine stimulates the cerebral cortex and respiration by acting on the brainstem and medulla.

Caffeine is found in many beverages, foods, over-the-counter medication, and prescription medications.

Caffeine is found in Anacin, Excedrin, Cafergot, Fiorinal, and Midol.

30
Q

Analeptics:

Define & provide example

A

Analeptics have a similar effect on the brain stem and medulla as caffeine.

  1. analeptic typically refers to respiratory analeptics.
  2. Analeptics are central nervous system stimulants that include a wide variety of medications used to treat:
    a. depression
    b. attention deficit hyperactivity disorder,
    c. respiratory depression.
    d. used as convulsants, with low doses causing patients to experience:
  3. heightened awareness
  4. restlessness
  5. rapid breathing.
31
Q

Anorexiants:

A

Anorexiants inhibit appetite by stimulating the cerebral cortex and the hypothalamus.

They have a stimulant effect on the hypothalamic and limbic regions, which control satiety. Anorexiants are used as therapy for obesity.

Anorexiants can produce psychological dependence. A patient can build a tolerance to the therapeutic effect of anorexiants, which may result in withdrawal symptoms if discontinuing anorexiant use abruptly.

32
Q

Amphetamines, analeptics, and anorexiants stimulate the release of What?

A

Amphetamines, analeptics, and anorexiants stimulate the release of:

norepinephrine and dopamine from the brain and from the peripheral nerve terminals of the sympathetic nervous system, resulting in euphoria and increase alertness.

Patients can experience:

sleeplessness, restlessness, tremors, irritability, and cardiovascular problems (increase heart rate, palpitations, dysrhythmias, and hypertension).

33
Q

Anorexiants and Analeptics include:

name 4:

A
  1. Benzphetamine (Didrex)
  2. Diethylpropion (Tenuate)
  3. Fenfluramine (Pondimin)
  4. Phentermine (Pheneturide)
34
Q

Amphetamine-Like Drugs:

A

Use For :

ADD and ADHD; Narcolepsy and treatment of Secondary depression

Half-life: 2–4 hours

Onset: 2 hours

Peaks: 3 hours

Duration: 8–12 hours

Ex: Methylphenidate HCl (Ritalin, Concerta) CSS II

Route: PO, IV

Pregnancy category: C

Pharmacokinetic: Incompletely absorbed from GI tract; metabolized in liver; excreted in urine and feces via biliary system

35
Q

Amphetamine-Like Drugs:

MOA:

A
  1. Blocks reuptake mechanisms of dopaminergic neurons.
  2. Decreases motor restlessness
  3. enhances ability to pay attention
  4. increases motor activity,
  5. increase mental alertness
  6. diminishes sense of fatigue, enhances spirit
  7. produces mild euphoria.
36
Q

Amphetamine-Like Drugs:

Adult dose:

Administration:

Ratalin

A

• Ritalin PO 2.5–5 mg before breakfast and lunch; may increase by 5–10 mg/day at weekly intervals for a maximum dose of 60 mg/day

Adm: Before Meals

37
Q

Amphetamine-like drugs:

Concerta

A

• Concerta: Initially, PO 18 mg once daily; may increase by 18/mg/day at weekly intervals to maximum dose of 54 mg/day

Adm: Before meals

Concerta contains methylphenidate

38
Q

Prevention

6 medication categories prescribed to prevent Migraines

A

1. Blood vessel constrictors

a. Methysergide— is particularly effective, however there are side effects that might make this drug less tolerable.

2. Blood vessel dilators

3. Antiseizure:

a. Divalproex sodium
b. Topiramate

4. Antidepressants:

a. Amitriptyline

b. Bupropion
c. Cyproheptadine

d. Fluvoxamine
e. Imipramine

5. Beta-blockers:

a. Propranolol

b. Timolol
c. Diltiazem

6. Analgesics:

a. Ibuprofen

39
Q

Symptom Management for Migraines

Name: 7

A

Symptom Management:

  1. Antiemetics
  2. Ergot alkaloids
  3. Nonsteroidal anti-inflammatory drugs (NSAIDs)
  4. Analgesics
  5. Nonopioids
  6. Opioids
  7. Triptans
40
Q

ERGOT ALKALOIDS

A

Dihydroergotamine and ergotamine belong to the group of medicines known as ergot alkaloids. They are used to treat severe, throbbing headaches, such as migraine and cluster headaches.

Ergot alkaloids are a large group of compounds produced by fungi that attack a wide variety of grass species, including small grains, during the growing season. These compounds are chemically divided into the clavine alkaloids, lysergic acids, simple lysergic acid amides and peptide alkaloids.

41
Q

ERGOT ALKALOIDS

USE:

A

Use: A first-line drug for treatment of an acute migraine attack.

Half-life: 21 hours

Onset: 1.5 hours

Peaks: 2 hours

Duration: 8 hours

42
Q

Ergot Alkaloids (for Migraines)

Provide:

Example/Route/Pharmacokinetic/MOA

A

Ex: Dihydroergotamine (DHE, Ergomar; with caffeine Cafergot)

Route: IM, SC, Intranasal

Pregnancy category: C

Pharmacokinetic: Slow incomplete absorption from GI tract; metabolized in liver; excreted in feces.

MOA: May have agonist/antagonist actions with alpha adrenergic, serotonergic, dopaminergic receptors.

  • Directly stimulates vascular smooth muscle, constricting arteries and veins.
  • May inhibit reuptake of norepinephrine.
43
Q

Ergot Alkaloids

Adult dose:

Admin:

A
  • The IM (intramuscular) or subcutaneous dose is 1 mg at onset and may repeat at hourly intervals, up to three injections daily.
  • Intranasal dose is 2 mg, one spray in each nostril; repeat in 15 minutes, up to 3 mg daily
  • Administer at first sign of migraine.
44
Q

Ergot Alkaloids: Contraindications

A

• Peripheral vascular disease, impaired renal/hepatic function, severe pruritus, coronary artery disease, hypertension, sepsis, malnutrition

contraindication is a condition or factor that serves as a reason to withhold a certain medical treatment due to the harm that it would cause the patient

45
Q

Ergot Alkaloids: Side effects/adverse reactions

A
  • Side effects: Cough and dizziness
  • Adverse effects: Prolonged administration or excessive dosage may produce ergotamine poisoning—nausea, vomiting, weakness of legs, pain in limb muscles, numbness and tingling of fingers/toes, precordial pain, tachycardia or bradycardia, hyper/hypotension.
  • Localized edema itching because of vasoconstriction of peripheral arteries and arterioles.
  • Feet, hands will become cold, pale, and numb.
  • Muscle pain occurs when walking and later even at rest.
  • Gangrene may occur. Occasionally confusion, depression, drowsiness, and convulsions appear.
46
Q

SEROTONIN AGONISTS:

TRIPTANS: Use/Example/Route

A

Use: Relief of migraine pain

Half-life: 2 hours

Onset: 1 hour

Peaks: 2 Hrs

Duration: 12 hours

Example: Sumatriptan (Imitrex)

Route: PO, SC, Intranasal

Pregnancy category: C

47
Q

SEROTONIN AGONISTS:

TRIPTANS:

Pharmacokinetic/MOA

A

Pharmacokinetic: metabolized in liver and excreted in the urine

How it works: • Binds selectively to vascular receptors producing a vasoconstrictive effect on cranial blood vessels

48
Q

SEROTONIN AGONISTS:

TRIPTANS: Adult dose / Administration

A

Adult dose:

• SC: 6 mg no more than two 6 mg injections within a 24-hour period and separated by at least 1 hour between injections

• PO: 50 mg maximum single dose 100 mg; may repeat no sooner than 2 hours with a maximum of 200 mg/24 hours

• Nasal: 5–20 mg may repeat in 2 hours; maximum 40 mg/24 hours

Administration: at first sign of migraine

49
Q

SEROTONIN AGONISTS:

TRIPTANS: Contraindications:

A

Contraindications: IV use; ischemic heart disease; silent ischemia, Prinzmetal’s angina, uncontrolled hypertension, concurrent ergotamine-containing preparations, hemiplegic or basilar migraine

• Caution with liver and kidney problems

50
Q

SEROTONIN AGONISTS:

TRIPTANS: Side effects / adverse reactions:

A

Side effects/ adverse reactions:

• Frequent: Oral—tingling, nasal discomfort; SC—injection site reactions, tingling, warm, hot sensation, dizziness, vertigo; Nasal—bad, unusual taste, nausea and vomiting

• Occasional: Flushing, weakness, visual disturbances; SC—burning sensation, numbness, chest discomfort, drowsiness, weakness; Nasal—discomfort of nasal cavity/throat, dizziness

• Adverse effects: Excessive dosage may produce tremor, redness of extremities, reduced respirations, cyanosis, convulsions, paralysis. Serious arrhythmias occur rarely but particularly in those with hypertension, obesity, smokers, diabetes, and those with strong family history of coronary artery disease.

51
Q

SEROTONIN AGONISTS:

TRIPTANS: Other Ex of Triptans (6)

A
  1. Almotriptan
  2. Eletriptan
  3. Frovatriptan
  4. Naratriptan
  5. Rizatriptan
  6. Zolmitripta

(MUL) Pharmacology (18 decks)

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