U2.1 Receptor-Based Pharmacology Flashcards

1
Q

CNS

A

Central Nervous System: brain & spinal cord

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2
Q

PNS

A

Peripheral Nervous System: - Nerves that carry messages to and from the CNS.
Two divisions: Somatic & Autonomic

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3
Q

Somatic Nervous System

A

Voluntary control over skeletal muscles. (component of PNS)

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4
Q

Autonomic Nervous System

A

Involuntary control over vital functions of the cardiovascular, digestive, respiratory, & genitourinary systems.
Two division: Sympathetic & Parasympathetic

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5
Q

Main activities of Autonomic Nervous System

A
  • Contraction of smooth muscle of the bronchi, blood vessels, GI tract, eye, and GU tract.
  • Contraction of cardiac muscle
  • Secretions of salivary, sweat, & gastric glands.
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6
Q

Sympathetic Nervous System

A

“Fight or Flight” Response
• Brain → Increased alertness & readiness
• Cardiovascular → Increased heart rate & blood pressure
• Musculoskeletal → Ready for sudden, intense physical activity
• GI → Liver produces more glucose for energy. Decreases peristalsis.
• Respiratory → Dilation of bronchi, increased respirations.
• Pupils → Dilation, increased vision.
• Integumentary → Warm, increased perspiration.
• GU → Decreased urine formation.

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7
Q

Parasympathetic Nervous System

A

“Rest & Digest” Response
• GI → Increased secretions, peristalsis.
• Cardiovascular → Decreased HR and BP.
• Respiratory → Constriction of bronchi, decrease in respirations

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8
Q

Acetylcholine (ACh)

A

Widely distributed in CNS; a major transmitter in ANS
CNS: May be excitatory or inhibitory; controls voluntary skeletal muscle movement
ANS: Activates the parasympathetic nervous system
Clinical significance: Myasthenia gravis, Alzheimer’s disease

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9
Q

Norepinephrine (NE)

A

Widely distributed in CNS; a major transmitter in ANS
CNS: May be excitatory or inhibitory
ANS: Activates the parasympathetic nervous system
Clinical significance: Depression, memory, panic attacks

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10
Q

Glutamate

A

CNS - Most common excitatory CNS neurotransmitter

Clinical significance: Memory

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11
Q

Gamma amiobutyric acid (GABA)

A

CNS - Most common inhibitory CNS neurotransmitter

Clinical significance: Seizure & anxiety disorders

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12
Q

Dopamine

A

basal ganglia & limbic system - Usually excitatory; locomotion, attention, learning, & reinforcing effects of abused drugs
Clinical significance: Parkinson’s disease; psychoses; motivation, pleasure

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13
Q

Endorphins & Enkephalins

A

Widely distributed in CNS and PNS - Usually inhibitory, reduction of pain.
Clinical significance: Opiods bind to endorphin receptors.

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14
Q

Serotonin

A

Common in brainstem, but also found in limbic system - Usually inhibitory.
Clinical significance: Anxiety, bipolar disorders, depression

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15
Q

Why is synaptic conduction highly selective?

A
  1. Synapses at different sites employ different transmitters.
  2. Many transmitters have more than one receptor.
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16
Q

Do most neuropharmacologic agents act by altering axonal transmission or synaptic transmission?

A

synaptic transmission

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17
Q

synaptic transmission

A

Synapses occur due to an electrical impulse. There is a release of neurotransmitters (chemical messengers) these cross the synapse to activate receptors.

  1. Transmitter synthesis
  2. Transmitter storage:
  3. Transmitter release
  4. Receptor binding
  5. Termination of transmission
18
Q

General mechanisms of ANS drugs

A
  • Synthesis of the neurotransmitter in the preganglionic neuron
  • Prevention of storage of the neurotransmitter in vesicles within the preganglionic nerve.
  • Influencing the release of the neurotransmitter from the preganglionic nerve.
  • Bind to the neurotransmitter receptor site on the postganglionic nerve.
  • Alters termination of transmission by preventing the normal destruction or reuptake of the neurotransmitter.
19
Q

General mechanisms of CNS drugs

A
  • Activation - stimulates firing of neurons
  • Inhibition – suppresses firing of neurons
  • Some have both actions
20
Q

muscarinic receptors

A

Ach
Parasympathetic targets: organs other than heart
Stimulatory –> smooth muscle and exocrine gland secretion
Inhibitory –> heart rate and force of contraction

21
Q

nicotinic receptors

A

Ach
Sympathetic & Parasympathetic
Postganglionic neurons & neuromuscular junctions of skeletal muscle
Stimulatory –> Smooth muscle & gland secretions
Nicotinic M –> Stimulates contraction of skeletal muscle

22
Q

How is Ach removed from the synaptic cleft?

A
  1. Acetylcholinesterase (AchE)

2. Pseudocholinesterase

23
Q

acetylcholinesterase

A

Enzyme in synaptic cleft, breaks down Ach - some drugs alter levels of AchE

24
Q

pseudocholinesterase

A

Found in liver. AKA plasma cholinesterase. Breaks down Ach. Some people have genetically altered levels making them unable to break down certain drugs in the plasma.

25
Q

Alpha1 receptors

A
Neurotransmitters: Epi, NE, Dopamine
ALL sympathetic target organs EXCEPT heart.
- Vasoconstriction
- Ejaculation
- Contraction of bladder neck & prostate
- Constriction of skin, mucous membranes
- Pupil dilation
26
Q

Alpha2 receptors

A

Neurotransmitters: Epi, NE, Dopamine
Presynaptic adrenergic nerve terminals, NOT in organs.
- Regulates NE release
- Can help reduce transmitter release when too much has accumulated in the synaptic cleft

27
Q

Beta1 receptors

A

Neurotransmitters: Epi, NE, Dopamine
Heart
- Increases HR
- Increases force of contraction
- Increases velocity of conduction in AV node
Kidneys
- Renin release (renin promotes synthesis of angiotensin which is a vasoconstrictor)

28
Q

Beta2 receptors

A

Neurotransmitter: Epi
ALL sympathetic target organs EXCEPT heart
- Bronchial dilation
- Decreased peristalsis
- Decreased urine production
- Glycogenolysis (increases glucose)
- Enhanced contraction of skeletal muscle
- Vasodilation in heart, lung, skeletal muscle

29
Q

Dopamine receptors

A

Neurotransmitter: Dopamine

  • Has much more effect in CNS
  • Dilates renal blood vessels
  • Increased force of cardiac contraction
30
Q

How is action of NE terminated?

A
  • 50 - 80% taken back into pregang nerve –> repackaged in vesicles for future use
  • remainder - destroyed by enzymes: MAO & COMT (in kidneys & liver)
31
Q

Classification of a drug that stimulates the sympathetic nervous system?

A

sympathomimetics, adrenergic-agonists

32
Q

Classification of a drug that stimulates the parasympathetic nervous system?

A

parasympathomimetics, muscarinic agonists

33
Q

Classification of a drug that inhibits the sympathetic nervous system?

A

adrenergic antagonists or blockers

34
Q

Classification of drugs that inhibit the parasympathetic nervous system?

A

anticholinergics, parasympatholytics, muscarinic blockers

35
Q

cholinergic synapses

A
  • Ach
  • stimulatory
  • distributed in CNS
  • motor cortex, basal ganglia
  • Parkinson’s, Alzheimer’s, Myasthenia gravis
36
Q

adrenergic synapses

A
  • NE
  • excitatory or inhibitory
  • heightens alertness, prominent while awake
  • depression, anxiety, panic, memory
37
Q

dopaminergic synapses

A
  • dopamine
  • generally excitatory
  • arousal & wakefulness
  • basal ganglia, limbic system
  • mechanism of cocaine, amphetamines, possibly marijuana
38
Q

endorphins & enkephalins

A
  • CNS & peripheral nervous system
  • hypothalamus, pituitary, limbic, spinal cord
  • opioid receptor –> affects pain transmission
39
Q

gamma aminobutyric acid (GABA) synapses

A
  • distributed in CNS
  • most commonly inhibitory
  • found t/o brain - basal ganglia, hypothalamus
  • seizure, anxiety
40
Q

glutamate synapses

A

glutamate receptor subtypes: N-methyl, D-aspartate

  • distributed in all areas of brain
  • ALWAYS excitatory
  • death of neurons in high amounts (can be a cause of toxicity)
  • memory
41
Q

serotonergic synapses

A
  • brainstem & limbic system
  • 98% of these are found outside CNS in platelets, mast cells GI tract
  • Low levels assoc. with anxiety, impulsivity, suicidal ideation.
  • synthesizes melatonin
42
Q

role of blood brain barrier

A
  • allows for continuous flow of glucose and oxygen
  • protects from pathogens or toxins
  • capillaries not as porous as in other parts of the body
  • form a tight barrier to many substances