Neuropharm Flashcards
1
Q
Cholinergic
A
refers to ACh
2
Q
Preganglionic transmission of both divisions
A
ACh primary transmitter; acts on nicotinic receptors, causes release of epinephrine
3
Q
Postganglionic parasympathetic fibers
A
ACH primary transmitter, acts on muscarinic receptors
4
Q
Postganglionic Sympathetic fibers
A
Norepinephrine (NE) primary transmitter relased
Exception = ACh at sweat glands, dopamine in kidneys
5
Q
Catecholamines
A
Norepi (NE)
Dopamine (DA)
Epinephrine (E)
6
Q
Adrenergic
A
Refers to NE, E, DA
7
Q
Catecholamine Synthesis
A
Tyrosine DOPA Dopamine Norepinephrine Epinephrine
8
Q
ACh in Cardiovascular system
A
Vasodilation, Negative chronotrope (rate) Negative inotrope (force) Negative domotrope (conduction velocity)
9
Q
ACh in Respiratory tract
A
Bronchoconstriction
Increased secretion
Stimulation of carotid and aortic bodies
10
Q
ACh in Urinary tract
A
Detrusor muscle contraction
Increased voiding pressure
Ureteral peristalsis
11
Q
ACh in GI tract
A
Increased tone
Increased amplitude of contractions/peristalsis
Increased secretions in stomach and intestine
12
Q
ACh additional effects
A
Miosis (pupil constriction)
Increased lacrimal, nasopharyngeal, salivary secretions
Increased production of sweat
Increased secretions all around!
13
Q
SLUDGE
A
Salivation Lacrimation Urination Defecation Gut pain/contraction Emesis
14
Q
BBM
A
Bronchospasm
Bronchorrhea (increased secretions in the bronchus)
Miosis
15
Q
Muscarinic Agonists
A
Ach Methacholine Carbachol Bethanechol Muscarine Pilocarpine
16
Q
Acetylcholine (Miochol-E)
A
Poor oral absorption
Used topically to produce miosis immediately after lens placement in cataract surgery
17
Q
Methacholine (Provocholine)
A
Administered by inhalation to diagnose bronchial airway hyperactivity
Contraindicated in patients using beta-blockers (bb’s can induce some bronchoconstriction)
Onset 1-4 mins, duration 15-75
18
Q
Bethanechol (Urecholine)
A
Treatment of urinary retention
Taken 3-4x daily on an empty stomach
19
Q
Carbachol (Isopto Carbachol, Miostat)
A
Causes miosis during surgery
Reduces intraocular pressure in glaucoma
20
Q
Pilocarpine (Salagen oral, Isopto Carpine opthalmic)
A
Non-selective muscarinic agonist (side effects with oral)
Treatment of xerostomia (dry mouth) due to radiation
Sjogren’s syndrome (decreased ability to produce salivation, lacrimation)
21
Q
Cevimeline (Evoxac - oral)
A
More selective - high affinity ofr lacrimal and salivary muscarinic receptors
Less GI upset than pilocarpine
22
Q
Muscarinic Agonists - Adverse Effects
A
Sweating Diarrhea, cramping Nausea, vomiting Sensation of tightness in bladder Visual disturbances Hypotension
Route of administration dictates side effects!!!!
23
Q
Muscarinic Agonists - General Precautions
A
- Asthma, COPD (bronchoconstriction)
- Urinary obstruction
- GI obstruction
- Cardiovascular disease w/ hypotension, bradycardia
- Hyperthyroidism
- Acid-peptic disease
24
Q
Muscarinic Antagonists
A
Bind muscarinic receptors and block Ach
Have little to no effect for nicotinic subtype
25
Atropine effects
Red as a beet, dry as a bone, blind as a bat, hot as a firestone, and mad as a hatter
26
Muscarinic Antagonist Cardiovascular effects
positive chronotropy (blood pressure unaffected)
Used for Vasovagal syncope and Asystole
27
Musc. Antagonist Respiratory effects
decreased bronchoconstriction
decreased secretions
Ipratropium, tiotropium (Spiriva)
28
Musc. Antagonist Eye effects
Mydriasis( dilation of pupils) long lasting
29
Musc. Antagonist GI tract effects
Antispasmodic, decrease acid secretion, decreased tone, amplitude and frequency of peristalsis
30
Musc. Antagonist other effects
Decreased salivation and nasal secretion.s
| Decreased tone in urinary tract
31
Musc. Antagonists and CNS
Motion sickeness
| Decrease extrapyramidal side effects of Parkinsons treatment
32
Musc. Antagonists and GU tract
For overactive bladder
Oxybutin - CYP3A4; lots of side effects
Tolterodine- more specific for bladder; CYP2D6
Trospium - only one eliminated significantly by kidneys
33
Muscarinic Antagonists Adverse Effects
Xerostomia
Constipation
Blurred vision
Cognitive impairment/feel fuzzy
34
Muscarinic Antagonists - Caution
Benign prostatic hyperplasia
GI obstruction
Urinary obstruction
Angle-closure glaucoma
35
Acetylcholinesterase Inhibitors
Also called anticholinesterases
Prevent breakdown of ACh
Increase ACh concentrations
36
Acetylcholinesterase Inhibitors - Therapeutic Uses
- Atonic bladder and GI tract
- Glaucoma
- Reversal of neuromuscular blockade
- Myasthenia gravis
- Alzheimer's disease (CNS issue)
37
Neostigmine
Relief of acute pseudo-colonic obstruction and/or post-op urinary retention
(Paralytic Ileus and Atony of the Urinary Bladder)
38
Anticholinesterase - Glaucoma
Contraction of ciliary muscle allows aqueous humor to flow out, decreasing intraocular pressure. Can be used, but not first choice.
39
Tensilon Test
To diagnose Myasthenia Gravis - an autoimmune neuromuscular disorder characterized by significant skeletal muscle weakness; appears to result in decrease in ACh receptors
40
Myasthenia Gravis Treatment
Physostigmine q2-4h
Neostigmine q3-6h
Ambenonium q3-8h
Short acting drugs! have to be given constantly.
41
Organophosphates
80% of pesticide-related hospitalizations
Responsible for over 200k deathers per year worldwide
SLUDGE will be apparent
Respiratory failure d/t hypersecreting
42
Tx of Organophosphate Poisoning
Administer Atropine and pralidoxime STAT
| Remove clothing, wash with soap and water, rinse eyes, maintain airway, do not induce vomiting!
43
Sympathomimetic Actions
1. Peripheral excitation on smooth muscle (skin, kidney, mucous membranes)
2. Peripheral inhibition on smooth muscle (gut and bronchial)
3. Cardiac excitiation
4. Metabolic (glycogenolysis)
5. Endocrine (renin, insulin, pituitary hormone)
6. CNS (resp stimulation, increased psychomotor activity and wakefulness)
44
Isoproteronol
A pure beta-agonist developed in 1940 with the benefit of no alpha activity. It is more potent than epinephrine at sites where both bind.
45
Direct-acting Adrenergic Agonist
acts directly on adrenergic receptors (may be highly selective for their receptor; alpha or beta)
46
Indirect-acting Adrenergic Agonist
availability of NE is increased via forcing the release of NE from storage vesicles or blocking uptake or metabolism
47
Mixed-acting Adrenergic Agonists
Will share features of both direct and indirect; ephedrine works at receptor and also increases release of NE
48
Therapeutic Uses of Sympathomimetics
Shock, hypotension, hypertension, arrhythmias, CHF, asthma, allergic rxns, opthalmic, narcolepsy, weight reduction, ADD/ADHD, local vascular and mucosal shrinkage
49
Epinephrine - vascular effects
Potent Vasopressor
+ inotrope
+chronotrole
peripheral vasoconstriction
50
Epinephrine - Cardiac effects
Used in cardiac arrest
- direct B1 agonist
- increased heart rate, cardiac output, O2 consumption
- Cardiac efficiency decreases
51
Epinephrine - Smooth muscle effects
- Gut relaxation
- Bladder sphincter contraction
- Uterine contraction in non-preg, relaxation in near-term pregnancy
52
Epinephrine - Respiratory effects
- Strong B2 agonist
- Bronchodilation
- Useful in resp support of anaphylaxis, angioedema, asthma
53
Epinephrine - Metabolic effects
- predominant inhibition of insulin release
- Increased glucose production (glucagon production and glycogenolysis)
- breakdown of adipose tissue
54
Epinephrine - Side efects
```
Headache
Tremor
Palpitations
Restlessness
Cerebral hemorrhage (if bp too high)
Arrhythmias
```
55
Norepinephrine - Cardiovascular effects
Strong periph vasoconstriction (due to no opposition from B2)
+Chronotrope
+inotropy in ventricles
Used for BP support in intensive care and shock - hospital only drug!
56
Norepi receptors
slighly less potent than Epi at a receptors, equipotent at B1, and no appreciable effects at B2
57
Norepi - Drug Interactions
MAOI
Antihistamines
Tricyclic antidepressants
58
Norepi - Caution
Extremem hypertension may result
| Extravasation (drug outside vein) can cause sloughing and necrosis
59
Dopamine
Used in the management of shock. That's it.
Only IV, does not cross BBB
60
Dopamine - receptors
Dopamine receptors
| B1 receptors
61
Dopamine - Side effects
Increased sympathetic activity
| Nausea, vomiting, headache
62
Dopamine - Caution
Adjust dose if patient is taking MAOI
| Beta-blockers interfere with cardiac effects
63
Isoproteronol - receptors
Beta selective, no alpha activity
64
Isoproteronol - Cardiovascular effects
Strong vasodilator
+inotrope
+chronotrope
+cardiac output
Used to treat some arrhythmias and bradycardia; largely been replaced
65
Isoproteronol - side effects
headache, palpitations, flushing, tachycardia
66
Dobutamine
Selective B1 agonist
67
Dobutamine - Cardiovascular
Inotrope > Chronotrope
Increases output
Useful in cardiac decompensation after surgery and CHF
68
Dobutamine Charge
CHF patient can receive infusion at hospital and have improved cardiac output for months
69
Beta-2 Selective Agonists
In treatment of COPD and asthma, we want to minimize cardiac effects while producing bronchodilation
70
Albuterol (Proventil, Proair, Ventolin)
SABA
Inhalation - dilation occurs w/in 15 mins, lasts 3-4h
Primary s/e = jittery or tachycardic
71
Terbutaline
B2 selective agonist
Used via inhalation or IV for status asthmaticus
also used as tocolytic in preterm labor
72
Long Acting Beta-2 Agonists (salmeterol, formoterol, advair)
- Duration of action >12h
- Tachyphylaxis is concern
you have an acute issue, use SABA, but already have LABA on board
73
Alpha-1 selective adrenergic receptor agonists
Effects of these drugs are d/t activation of a adrenergic receptors in vascular smooth muscle
-blood pressure goes up or is maintained, so they are useful for patients with hypotension or shock
74
Phelnylephrine
- a-1 selective adrenergic receptor agonist
- activates Beta receptors at high concentrations
- when given IV, marked arterial vasoconstriction
- also nasal decongestant and mydriatic
75
Alpha-2 Selective Adrenergic Receptor
Used in treatment of hypertension - activates alpha-2 receptors in CNS which supress sympathetic activity
76
Clonidine
- a-2 selective
- originally tested as a nasal decongestant, found to cause hypotension, sedation, and bradycardia
- IV infusion causes opposite (rise in BP) than oral
77
Apraclonidine
- a-2 selective
| - used topically to reduce intraocular pressure
78
Bimonidine
- a-2 selective
- administered ocularly; lowers intraocular pressure
- use in caution with patients w/ cardiovascular disease (slight hypotension, sedation can occur)
79
Guanfacine
- a-2 selective
- More selective than Clonidine, works by same mechanism in brain stem
- Approved by FDA to treat ADHD in children age 6-17
80
Guanabenz
- a-2 selective
- Induces hypotension, sedation and bradycardia
- dose adjust in liver patients
81
Methyldopa
- a-2 selective
| - Metabolized by a-methylnorepinephrine in the brain which activates a-2 receptors and works similarly to clonidine
82
Tizanidine
- a-2 selective
| - Muscle relaxant, treats spasticity related to cerebral and spinal disorders
83
Amphetamine
- Misc. sympathomimetic agonist
- Schedule II - should only be used under medical supervision
- powerful CNS stimulant and has peripheral a and B actions
84
Amphetamine - Cardio
Raises both systolic and diastolic blood pressures.
| Arrhythmias may occur in large doses
85
Amphetamine - CNS
- one of the most potent drugs for stimulating the CNS
- Stimulates medullary respiratory center
- lessens central depression caused by other drugs
86
Amphetamine - Toxicity and Adverse Effects
- CNS effects: restlessness, dizziness, tremor, hyperactive reflexes, talkativeness, tenseness, irritability, weakness, insomnia, fever and sometimes euphoria
- headache, chills, pallor or flushing, palpitation, arrhythmias, angina, circulatory collapse, sweating, hyper or hypo tension
- dry mouth, anorexia, N/V/D
87
Amphetamine - Contraindications
Patients with anorexia, insomnia, asthenia, psychopathic personality, or a history of homicidal or suicidal tendencies
88
Methamphetamine
Chemically closely related to amphetamines and ephedrine. Releases DA and other amines in the brain, inhibits MAO.
89
Methylphenidate
Mild CNS stimulant; more mental than motor effects.
| Large doses may lead to convulsions
90
Ephedrine
- Agonist of both alpha and beta receptors
- Stimulates heart rate, CO, increase PVR => increases BP
- increased resistance to urinary flow, bronchodilation, CNS stimulation
91
Adrenergic Receptor Antagonists
Drugs that inhibit the interaction of NE, E and other drugs with alpha and beta receptors
- important for treatment of cardiovascular disease
92
Alpha Adrenergic Receptor Antagonists
Alpha-1: contraction of arterial, venous and visceral smooth muscle
Alpha-2: suppression of sympathetic output, increasing vagal tone, facilitating platelet aggregation, inhibit release of NE and ACh from nerves, regulation of metabolic effects (suppression of insulin secretion and inhibition of lipolysis)
93
Alpha-1 Receptor Antagonists
Blocking a-1 adrenergic receptors results in a fall of blood pressure; effects exaggerated if a-2 is blocked too
94
Prazosin
- alpha-1 receptor antagonist
- used to treat hypertension (CHF and BPH also)
- Adverse effects: hypotension and syncope
95
Alpha-2 Receptor Antagonists
Increase sympathetic outflow, cause release of NE from nerve endings
