M4 Flashcards
1
Q
VOLUNTARY control of skeletal muscle
A
SOMATIC NS
2
Q
INVOLUNTARY control of glands and smooth muscle
A
AUTONOMIC NS
3
Q
AUTONOMIC NS
FIGHT OR FLIGHT
A
SYMPATHETIC
4
Q
AUTONOMIC NS
REST AND DIGEST
A
PARASYMPATHETIC
5
Q
- subdivision of the peripheral effector nervous system
- composed of 2 motor neurons that connect the brain and effector organ
- govern involuntary activities such as heart beat, GI mobility, breathing, etc.
- usually controls the activity of the organs covered by a viscera, so is called the visceral division of the PNS (peripheral)
A
AUTONOMIC NERVOUS SYSTEM
6
Q
AUTONOMIC NS
subdivision of the ____ nervous system
A
peripheral effector
7
Q
AUTONOMIC NS
composed of ____ neuron that connect the brain and effector organ
A
2 motor neurons
8
Q
AUTONOMIC NS
usually controls the activity of the organs covered by a ____
A
viscera
9
Q
- explain the mechanism of impulse transport across the synapse
- presence of gaps or spaces
- nervous system is discontinuous
A
SYNAPTIC NEUROTRANSMISSION
10
Q
SYNAPTIC NEUROTRANSMISSION
explain the mechanism of ____ across the synapse
A
impulse transport
11
Q
SYNAPTIC NEUROTRANSMISSION
presence of gaps and spaces
A
synapse
12
Q
SYNAPTIC NEUROTRANSMISSION
nervous system is ____
A
discontinuous
13
Q
the region BETWEEN pre ganglion and post ganglion
A
ganglion
14
Q
SYNAPTIC NEUROTRANSMISSION
- synthesis, storage (vesicles), release or exocytosis of NT
- has enzymes: metabolism
- has autoreceptors: inhibitory effect
A
PRESYNAPSE
15
Q
SYNAPTIC NEUROTRANSMISSION
PRESYNAPSE:
auto receptors: ____ effect
A
inhibitory
16
Q
SYNAPTIC NEUROTRANSMISSION
parts of synapse
A
presynapse
cleft
post synapse
17
Q
SYNAPTIC NEUROTRANSMISSION
has enzymes: metabolism
A
cleft
18
Q
SYNAPTIC NEUROTRANSMISSION
- has the majority of receptors: excitatory effect
- enzymes: metabolism
A
POST SYNAPSE
19
Q
SYNAPTIC NEUROTRANSMISSION
POST SYNAPSE:
majority of receptors: ____ effect
A
excitatory
20
Q
SYNAPTIC NEUROTRANSMISSION
induces release or exocytosis
A
Calcium ion
21
Q
SUBDIVISION OF ANS
bronchioles of the lungs:
DILATION
A
SYMPATHETIC
22
Q
SUBDIVISION OF ANS
bronchioles of the lungs:
CONSTRCITION
A
PARASYMPHATETIC
23
Q
SUBDIVISION OF ANS
secretion of adrenaline and NA
A
SYMPATHETIC
24
Q
SUBDIVISION OF ANS
salivation
A
PARASYMPATHETIC
25
# **SUBDIVISION OF ANS**
____ responses dominate when the person is under **STRESS**, **EXERCISE**, or **IN MOTION** (such as running)
SYMPATHETIC
26
# **SUBDIVISION OF ANS**
____ dominates when the person is **AT REST (energy is conserved)**; during **sleep**
PARASYMPATHETIC
27
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
ORIGIN OF NEURONS:
**sympathetic**
T1-T12; L1-L5
Thoracolumbar NS
28
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
ORIGIN OF NEURONS:
**parasympathetic**
CN 3,7,9,10; S2-S4
Craniosacral NS
29
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
LENGTH OF NEURONS:
**sympathetic**
SHORT **pre** ganglion
LONG **post** ganglion
30
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
LENGTH OF NEURONS:
**parasympathetic**
LONG **pre** ganglion
SHORT **post** ganglion
31
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
LOCATION OF GANGLION:
**sympathetic**
near **spinal cord**
31
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
LOCATION OF GANGLION:
**parasympathetic**
near **effector organ**
32
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
**sympathetic**
**PRE** ganglion
ACETYLCHOLINE
32
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
**sympathetic**
**POST** ganglion
NOREPINEPHRINE
32
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
**parasympathetic**
**PRE** ganglion
Acetylcholine
32
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
**parasympathetic**
**POST** ganglion
Acetylcholine
32
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
**MAJOR/PRIMARY** NT of **PARASYMPATHETIC**
Acetylcholine
32
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
**MAJOR/PRIMARY** NT of **SYMPATHETIC**
NOREPINEPHRINE
33
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
RECEPTORS (POST SYNAPSE):
**sympathetic**
**GANGLION**
NICOTINIC NEURAL
(QISS)
34
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
RECEPTORS (POST SYNAPSE):
**sympathetic**
**EFFECTOR**
ADRENORECEPTORS
(a-1, b-1,2)
35
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
RECEPTORS (POST SYNAPSE):
**parasympathetic**
**GANGLION**
NICOTINIC NEURAL
(QIQ)
36
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
RECEPTORS (POST SYNAPSE):
**parasympathetic**
**EFFECTOR**
CHOLINORECEPTORS: muscarinic, nicotinic
37
# **SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES**
PARA | EFFECTOR:
**nicotinic** binds to ____
sodium channel
38
# **SYMPATHETIC VS PARASYMPATHETIC**
* **sweat glands**
more PRIMARILY parasympathetic but may part na sympathetic
39
# **SYMPATHETIC VS PARASYMPATHETIC**
**cardiac** and **smooth** muscle, **gland** cells, **nerve terminals**
PARA & SYMPA
40
# **SYMPATHETIC VS PARASYMPATHETIC**
**renal** vascular smooth muscle
SYMPATHETIC
41
# **SYMPATHETIC VS PARASYMPATHETIC**
**skeletal** muscle
SOMATIC
42
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
response related to **stress**
FIGHT OR FLIGHT
43
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
response during **basal conditions**
rest and digest
44
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
NE vs Ach
functional antagonist
(different targets, opposite effects)
45
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**heart**
tachycardia
46
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
**heart**
bradycardia
47
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**pupils**
mydriasis
48
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**NE**
Adrenergic nervous system
49
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
**ACh**
Cholinergic Nervous system
50
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
**pupils**
miosis
51
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**bronchi**
broncho**dilation**
52
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
**bronchi**
broncho**constriction**
53
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**GIT**
ILEUS: **loss** of peristalsis
54
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPHATETIC:
**GIT**
bowel movement
55
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**urinary bladder**
urine **retention**
56
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
**urinary bladder**
**urination**
57
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
SYMPATHETIC:
**sweating**
**APOCRINE**: palms & soles
58
# **SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE**
PARASYMPATHETIC:
**sweating**
**ECCRINE**: generalized for thermoregulation
59
* a **network** of **nerve fibers** within **intestinal walls**
* considered a **3rd division** of ANS
* a **large** and **highly organized** collection of neurons located in the **walls** of **GI** system
* includes **myenteric plexus** and **submucous plexus**
* PARAsympathetic **activates** ENS
* SYMPATHETIC **inhibits** ENS
ENTERIC NERVOUS SYSTEM
60
# **ENTERIC NERVOUS SYSTEM**
considered a ____ of ANS
3rd division
61
# **ENTERIC NERVOUS SYSTEM**
located in the
walls of GI system
62
# **ENTERIC NERVOUS SYSTEM**
includes ____ and ____
Myenteric Plexus
Submucous Plexus
63
# **ENTERIC NERVOUS SYSTEM**
PARASYMPATHETIC
activates ENS
64
# **ENTERIC NERVOUS SYSTEM**
SYMPATHETIC
inhibits ENS
65
# **ENTERIC NERVOUS SYSTEM**
**Myenteric Plexus** is also known as
Auerbach's Plexus
66
# **ENTERIC NERVOUS SYSTEM**
**Submucous Plexus** is also known as
Meissner's Plexus
67
# **ENTERIC NERVOUS SYSTEM**
MYENTERIC:
**location**
between the **circular** & **longitudinal** muscle layers of the **gut wall**
68
# **ENTERIC NERVOUS SYSTEM**
SUBMUCOUS:
**location**
**within** the **submucosa** of the **GI tract**
69
# **ENTERIC NERVOUS SYSTEM**
MYENTERIC:
**function**
controls **GI motility (peristalsis)** and **muscle contractions**
70
# **ENTERIC NERVOUS SYSTEM**
SUBMUCOUS:
**function**
regulates **secretions** and **blood flow** in the intestinal mucosa
71
# **ENTERIC NERVOUS SYSTEM**
MYENTERIC:
**neuronal composition**
contains **motor neurons** and **interneurons** controlling smooth muscle
72
# **ENTERIC NERVOUS SYSTEM**
SUBMUCOUS:
**neuronal composition**
composed of **sensory neurons** and **secretomotor neurons**
73
# **ENTERIC NERVOUS SYSTEM**
MYENTERIC:
**influence**
affects the **entire GI tract**, from the **esophagus - rectum**
74
# **ENTERIC NERVOUS SYSTEM**
SUBMUCOUS:
**influence**
more prominent in the **small** and **large** intestines
75
# **ENTERIC NERVOUS SYSTEM**
MYENTERIC:
**effect on digestion**
regulates **movement** of food through the gut
76
# **ENTERIC NERVOUS SYSTEM**
SUBMUCOUS:
**effect on digestion**
modulates **enzyme secretion** and **absorption** processes
77
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* **EXCITATORY** neurotransmitter
* stimulates smooth muscle **contraction**, increases **glandular secretions**
ACETYLCHOLINE
78
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* **INHIBITORY** (mostly sympathetic influence)
* decreases **motility** and **secretions**, contracts **sphincters**
NOREPINEPHRINE
79
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* modulates **GUT motility** and **secretion**
* stimulates **peristalsis**, affects **sensory neurons**, and regulates **secretion**
SEROTONIN
80
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* modulates **ENS neuronal activity**
* inhibitis **excessive motility**, reduces **Ach release**
DOPAMINE
81
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* **INHIBITORY neurotransmitter**
* **relaxes** smooth muscles, promotes **vasodilation**
NITRIC OXIDE
82
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* regulates **smooth muscles** and **secretions**
* **relaxes** gut muscles, increases **intestinal secretion**, and **dilation** of **blood vessels**
VASOACTIVE INTESTINAL PEPTIDE (VIP)
83
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* **EXCITATORY**, involved in **pain perception**
* stimulates smooth muscle **contraction**, enhances **pain signaling**
SUBSTANCE P
84
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* MODULATE **motility** and **pain perception**
* INHIBIT **peristalsis**, REDUCE **pain sensation**
ENKEPHALINS (opioid peptides)
85
# **ENTERIC NERVOUS SYSTEM | TRANSMITTERS**
* acts as a **neurotransmitter** in the **ENS**
* can INDUCE **muslce relaxation** and MODULATE **ENS signaling**
ATP (Adenosine Triphosphate)
86
# **SYMPATHETIC DRUGS**
Major NT
NOREPINEPHRINE
87
# **SYMPATHETIC DRUGS**
agonists
-mimetics
88
# **SYMPATHETIC DRUGS**
antagonists
-lytics
89
# **SYMPATHETIC DRUGS**
ENDOGENOUS catecholamines
Epinephrine,
Norepinephrine,
Dopamine
90
# **SYMPATHETIC DRUGS**
ENDOGENOUS CATECHOLAMINES:
**1st** to be synthesized
Dopamine
91
# **SYMPATHETIC DRUGS**
ENDOGENOUS CATECHOLAMINES:
**2nd** to be synthesized
Norepinephrine
92
# **SYMPATHETIC DRUGS**
ENDOGENOUS CATECHOLAMINES:
**3rd** to be synthesized
Epinephrine
93
synthesize **tyrosine** to **L-dopa**
tyrosine hydroxylase
94
**inhibits** tyrosine hydrxylase
METYROSINE
95
**inhibits** storage of dopamine
Reserpine / Tetrabenazine
96
**exocytosis** inhibitor in the presynapse
Bretyllium, Guanethidine
97
**reuptake** inhibitor (presynapse)
Cocaine
Tricyclic antidepressants
98
# **SYMPATHETIC DRUGS**
**biosynthesis** of endogenous catecholamine
Tyrosine -> L-dopa -> Dopamine -> Norepinephrine -> Epinephrine
99
# **SYMPATHETIC DRUGS**
**precursor** to the conversion of **L-dopa**
tyrosine
100
# **SYMPATHETIC DRUGS**
* the **rate limiting** enzyme in production of endogenous catecholamines
* inhibited by **Metyrosine** (decrease sympathetic effect)
TYROSINE HYDROXYLASE
101
# **SYMPATHETIC DRUGS**
Formation of **Dopamine**:
enzyme
L-DOPA carboxylase
102
# **SYMPATHETIC DRUGS**
Formation of **NE** occurs where
inside the **vesicles**
103
# **SYMPATHETIC DRUGS**
Formation of **NE**:
enzyme
Dopamine-B-hydroxylase
104
# **SYMPATHETIC DRUGS**
Formation of **Epinephrine** occurs in the ____
adrenal medulla
105
# **SYMPATHETIC DRUGS**
Formation of **Epinephrine**:
enzyme
PENMT: Phenylethanolamine-N-methyltransferase
106
# **SYMPATHETIC DRUGS**
PREVENT **premature metabolism** of dopamine
storage of dopamine
107
# **SYMPATHETIC DRUGS**
STIMULANTS of **exocytosis**
| greater for NE binding
Tyramine
Ephedrine
Amphetamine, Angiotensin II
Methamphenamine
| TEAM
108
# **SYMPATHETIC DRUGS**
INHIBITORS of **exocytosis**
| less NE for binding
Guanethidine
Guanadrel
Bretylium
| GGB
109
# **SYMPATHETIC DRUGS**
TERMINATION occurs in the ____
cleft
110
# **SYMPATHETIC DRUGS**
REDUCE NE for binding
Termination
111
# **SYMPATHETIC DRUGS**
REUPTAKE **inhibitors**
| increase NE for binding
Cocaine
Atomoxetine
Sibutramine
| CAS
112
# **SYMPATHETIC DRUGS**
enzymes for METABOLISM
Monoamine Oxidase (MAO)
Catechol-O-Methyltrasnferase (COMT)
113
# **SYMPATHETIC DRUGS**
PRODUCTS of metabolism:
**EPI, NE**
3-methoxy-4-hydroxymandelic acid or VMA (vanillylmandelic acid)
114
# **SYMPATHETIC DRUGS**
PRODUCTS of metabolism:
**DOPAMINE**
homovanillic acid
115
# **SYMPATHETIC DRUGS**
MAO inhibitors
MPITS
116
# **SYMPATHETIC DRUGS**
COMT inhibitors
-capones
117
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
GPCRs
QISS Alpha receptors
Type 2 metabotropic receptors
118
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**smooth muscle**
contraction
119
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**blood vessel**
vasco**constriction**
| increase BP
120
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**bladder trigone**, **sphincter CLOSURE**
urine **retention**
121
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**prostatic smooth muscle**
contraction = urine retention
122
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**radial muscles (iris)**
contraction = MY**D**RIASIS
123
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**sphincter muscle**
| contraction of iris
bigger pupils -> MIOSIS
124
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 1:
**pilomotor smooth muscles (skin)**
PILOERECTION (goosebumps)
125
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
* **inhibits** further release of NE from the vesicles
* **less** NE for binding
* CONSEQUENCES:
* Central: **depression**, **sedation**
* Peripheral: **vasodilation** = decrease BP (anti HTN = a2 agonist)
ALPHA 2 receptor; PRESYNAPTIC = inhibitory
126
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 2:
**POST** synaptic
**Peripheral blood vessel** (usually in the eyes)
VASOCONSTRICTION
127
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 2:
* reduces **pain perception** via effects on the spinal cord and brain stem
* used in **chronic pain** and **surgical anesthesia**
ANALGESIC
128
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 2:
* helps manage **opioid** and **nicotine withdrawal** by decreasing sympathetic overactivity
Reduction of Opiate Withdrawal Symptoms
129
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
ALPHA 2:
* some **a2 agonists** reduce **aqueous humor production**, lowering **intraocular pressure** in **glaucoma**
decreased Intraocular pressure
130
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
* HEART = increase **inotropy**, **chronotropy**, **dromotropy** = **cardiac stimulation**
* KIDNEY = increase **renin**
BETA 1 receptor
131
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 1:
important for synthesis of **angiotensin II** = **increase BP**
RENIN
132
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 1:
* **specific region** with beta 1 receptor
* specific region where **beta 1** are
JUXTAGLOMERULAR APPARATUS
133
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 2:
**smooth muscles**
relaxation
134
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 2:
**bronchi**
broncho**dilation**
135
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 2:
**uterus**
tocolysis
(relaxation of uterus)
136
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 2:
**blood vessels (skeletal muscles)**
vasodilation
137
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 2:
**skeletal muscles contraction**
tremors
138
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 2:
**skeletal muscle** ____ iptake in the muscles = **hypokalemia**
enhance K ion uptake
## Footnote
low levels of K ion in the blood leads to hypokalemia
139
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 3:
**fat cells**
adipocytes
140
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
BETA 3:
**break down of fats**
lipolysis
| weight loss
141
# **SYMPATHETIC DRUGS | ADRENORECEPTORS**
**activation** of BETA 3 leads to
lipolysis
142
# **SYMPATHETIC DRUGS**
agonists
SYMPATHOMIMETICS
143
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS**
**adrenoceptor activation**: drug binding to receptor
DIRECT acting sympathomimetics
144
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS**
* **enhance** level of NE for binding
* enhance **exocytosis**
* inhibit **reuptake**
INDIRECT acting sympathomimetics
145
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS**
**direct + indirect**
enhance exocytosis
MIXED ACTING sympathomimetics
146
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS**
* Nonselective
* Selective
Direct acting
147
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS**
DIRECT ACTING:
* activate **MORE THAN 1** sympathetic receptor (alpha and beta)
* **endogenous catecholamines**: EPI, NE, DA
NONSELECTIVE
148
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
* **high potency** at **adrenoreceptors**
* **high affinity** in **BETA** than alpha
* **beta** effect at **LOW** dose
* **alpha** effect at **HIGH** dose
* **Polar/Hydrophilic** -- **impermeable** BBB = no CNS effects
* extensively **metabolized** by MAO and COMT
NONSELECTIVE
149
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**high POTENCY** at ____
adrenoreceptors
150
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**higher AFFINITY** in ____ than ____
in **beta** than alpha
151
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**BETA** effect at ____ dose
LOW
152
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**ALPHA** effect at
____ dose
HIGH
153
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE DIRECT ACTING
EPI, NE, DA
154
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
* the ONLY **bronchodilating**
* **B1 = B2 >>> a1**
* the ONLY that has activity at **B2** = only bronchodilating endogenous
EPINEPHRINE
155
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**B1 > a1**
NOREPINEPHRINE
156
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**D1 > B1 >> a1**
DOPAMINE
157
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
* enhance **renal vasodilation**
* increase **GFR**
* increase **diuresis**
D1
158
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
____ BBB
Polar/Hydrophilic
Impermeable - cannot pass
NO CNS effects
159
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
extensively **metabolized** by
MAO and COMT
160
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**duration of action**
SHORT
161
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**oral bioavailability**
LOW
162
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
* **1ST LINE** **cardiac stimulant** (B-1)
* **1ST LINE** agent in the treatment of **anaphylactic shock** (caused by allergy)
* **1ST LINE** agent for: **anaphylaxis**, **anaphylactoid reaction**
* **Local vasoconstrictor** combined with LIDOCAINE = enhanced local anesthesia of lidocaine and minimize bleeding
* for **glaucoma**
EPINEPHRINE / ADRENALINE
163
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
**1ST LINE** for
cardiac stimulant
tx of anaphylactic shock
anaphylaxis
anaphylactoid
164
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
* increase **histamine** = broncho**constriction**
* **IgE** mediated
anaphylaxis
165
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
* increase **histamine** = broncho**constriction**
* **NON IgE** mediated; **drug induced**
* can be caused by: **Morphine**, **Tubocurarine**, **Guanethedine**
anaphylactoid
166
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
**local vasoconstrictor** combined with ____
LIDOCAINE
167
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | EPI/ADRENALINE:
* for **GLAUCOMA**
* **prodrug** of **EPI**
* **pivalic acid ester** of **EPI**
DIPIVEFRIN
168
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
**1ST LINE** for **SEPTIC SHOCK** (caused by infection)
NOREPINEPHRINE / NORADRENALINE / LEVARTERENOL
169
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE:
* **alternative** for **SEPTIC SHOCK** and **CARDIOGENIC SHOCK** (caused by HF)
* management of **ACUTE HF** with complication of **oliguria** and **anuria** (low urine output)
DOPAMINE
170
**LOW** urine output
oliguria & anuria
171
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | **TOXIC EFFECTS**:
**a1** overstimulation = **vascoconstriction**
HTN, digital necrosis (purple fingers, poisoning)
172
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | **TOXIC EFFECTS**:
**b1** overstimulation
ventricular tachycardia
173
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
NONSELECTIVE | **TOXIC EFFECTS**:
treatment for **b1 overstimulation = VENTRICULAR TACHYCARDIA**
PHENTOLAMINE
174
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE:
* **CONSTRICTOR** drugs
* Phenylephrine, Methoxamine
* Propylhexedrine
* Tetrahydrozoline, Oxymetazoline, Nafazoline
ALPHA1 AGONIST
175
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE:
**Alpha 1 agonist**
Phenyl**ephrine**, Metho**xamine**
Propylhex**edrine**
Tetrahydro**zoline**, Oxymeta**zoline**, Nafa**zoline**
176
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
effects
vasoconstriction
mydriasis
177
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**local** effects
intrasal
eye drops
178
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**nasal spray** - decongestant
Oxymetazoline (Drixine)
179
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**eye drops** - treatment of **red eyes**
Tetrahydroziline (Eye Mo Red)
180
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**systemic** effects
for **nasal congestion**
tx of **hypotension**
181
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**MYDRIATIC** in eye examination = for **full view** of **retina**
PHENYLEPHRINE
182
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**LOCAL** toxic effect
rhinitis medicamentosa
| rebound congestion if used **more than 3 days**
183
183
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 1 AGONIST**:
**SYSTEMIC** toxic effects
* increase blood pressure
* urine retention
184
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE:
* anti**glaucoma** agents: **Apraclonidine**, **Brimonidine**
* anti**hypertensive** agents: **Methyldopa**, **Clonidine**, **Guanfacine**, **Guanabenz**
ALPHA 2 AGONIST
185
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
anti**glaucoma** agents
Apraclo**nidine**, Brimo**nidine**
186
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
anti**hypertensive** agents
**Methyl**dopa, **Clo**nidine, **Guan**facine, **Guan**abenz
187
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
BRAND NAME **methyldopa**
Aldomet
188
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
BRAND NAME **Clonidine**
Catapres
189
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
* PRODRUG of **methyldopa**
* a **FALSE** NT
a-methyl-norepinephrine
190
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
MOA of **Clonidine**
Initial: increase BP
Final: decrease BP
191
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
CLINICAL USE **methyldopa**
HTN **emergency**
(increase in BP leads to **organ damage**)
| if NO organ damage -- HTN urgency
192
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
CLINICAL USE **Clonidine**
HTN crisis
(general increase in BP)
193
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
TOXIC EFFECTS **methyldopa**
Sedation
Hepatotoxicity
positive Coombs test
positive Hemolytic anemia
194
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
SELECTIVE | **ALPHA 2 AGONIST**:
TOXIC EFFECTS **Clonidine**
Withdrawal
Rebound HTN
195
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**NON**SELECTIVE **BETA AGONIST**:
* alternative agent during **shock**
* alternative in the management of **acute heart failure**
Isoproterenol / Isoprenaline
| na shock si TERE PRE! nagka heart failure
196
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 1 SELECTIVE AGONIST**:
* DIAGNOSIS: for **pharmacologic stress test**
* TREATMENT: **1st line** treatment for **cardiogenic shock** (caused by HF)
* used for management of **acute HF**
DOBUTAMINE
| DOB DOB - heart beat sound
197
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
SHORT ACTING
Terbutaline
Albuterol
Metaprotrenol
Pirbuterol
| TAMP
198
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
LONG ACTING
Salmeterol
Formoterol
Indacaterol
Bambuterol
| SFIB
199
199
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
short acting that is the ONLY **subcutaneous**
Terbutaline
200
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
brand name of **Albuterol**
Salbutamol
201
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
long acting that has **SLOW** onset
Salmeterol
| mabagal si SALM
202
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
long acting that has **FAST** onset
Formoterol
| mabilis ang MOTER (motor)
203
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
CLASSES
SABA
LABA
Tocolytics
203
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
the ONLY **oral** LONG ACTING
Bambuterol
204
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
* treatment of **preterm labor**
* relax **uterine smooth muscle**
TOCOLYTICS
205
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
TOCOLYTICS
Isoxsuprine (Duvadilan)
Ritodrine
Terbutaline
206
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
OFF LABEL **tocolytic**
Terbutaline
207
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING**
**BETA 2 SELECTIVE AGONIST**:
TOXIC EFFECTS
* Hyppokalemia
* **Ventricular tachycardia** (due to overdose -- can activate BETA 1)
208
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
* has **D/I** with **MAOI** = increase NE = **hypertensive crisis**
TYRAMINE
209
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
* from **Ma Huang**
Ephedrine
210
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
* alternative for **ADHD**
Amphetamine
211
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS
Tyramine
Ephedrine
Amphetamine
Metamphetamine
Modafinil
Methylphenidate
Phenmetrazine
| TEAM MMP
212
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
**shabu**
Methamphetamine
213
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
1st line agent for **narcolepsy**
Modafinil
214
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
1st line agent for **ADHD**
Methylphenidate
215
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
RELEASERS:
**anorexiant**
Phenmetrazine
216
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
REUPTAKE INHIBITORS:
ONLY **vasoconstrictor** local anesthetic
Cocaine
217
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
REUPTAKE INHIBITORS
Cocaine
Atomoxetine
Sibutramine
| CAS
218
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
REUPTAKE INHIBITORS:
alternative agent for **ADHD**
Atomoxetine
219
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
REUPTAKE INHIBITORS:
used in management of **obesity**, **discontinued** in the Philippines due to unnecessary cardiovascular risks to patients
Sibutramine
220
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
APPETITE SUPPRESSANT:
typically prescribed for **SHORT-TERM** weight loss
Phentermine
221
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
APPETITE SUPPRESSANT:
a **FAT ABSORPTION inhibitor** that helps with weight management
Orlistat (Xenical, Alli)
222
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
APPETITE SUPPRESSANT:
an **injectable** medication that regulates **appetite** and **caloric intake**
Liraglutide (Saxenda)
223
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING**
APPETITE SUPPRESSANT:
a **combination drug** that works on the **brain's hunger** and **reward centers** to reduce appetite
Naltrexone-Bupropion
(Contrave)
224
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | MIXED ACTING**
* tx for **nasal congestion**
* tx for **hypotension**
* **OTC appetite supressant**, but was **removed** from the market due to **hemorrhagic stroke** in **young women**
Phenylpropanolamine
225
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | MIXED ACTING**
why is **Phenylpropanolamine** removed from the market
due to hemorrhagic stroke in young women
226
# **SYMPATHETIC DRUGS | SYMPATHOMIMETICS | MIXED ACTING**
used for **hypotension**
Mephentermine
Metaraminol
227
# **SYMPATHETIC DRUGS**
ANTAGONISTS
SYMPATHOLYTICS
228
# **SYMPATHETIC DRUGS**
effect of SYMPATHOLYTICS
Parasympathetic effects
229
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
* **IRREVERSIBLE**, **NON**-competitive
* inhibit **alpha receptor**
* used in **PHEOCHROMOCYTOMA** (tumor in **adrenal medulla**) -- due to too much EPI
* **presurgical** treatment
* management of **HTN crisis** in **inoperable** tumor
* inhibit **histaminic** receptor
* used in **MASTOCYTOSIS** (too much muscle)
* inhibit **5-HT** receptor
* used in **CARCINOID SYNDROME** (tumor found in **enterochromaffin** cell)
* provide symptomatic release
PHENOXYBENZAMINE
230
1st line agent for **Carcinoid syndrome / Serotonin syndrome**
Cyproheptadine
231
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
* **REVERSIBLE**, **COMPETITIVE**
* tx of **sympathomimetic poisoning**
* management of **pheochromocytoma**
* tx of **Raynaud syndrome** (digital necrotic due to **extreme climate**)
* used in the treatment of **erectile dysfunction** (safer bc locally injected)
PHENTOLAMINE
232
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
**-zosins**
ALPHA 1 SELECTIVE BLOCKERS
233
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
**ALPHA 1 SELECTIVE BLOCKERS**:
* **Vasodilators** - antihypertensives
* causes **1st dose phenomenon** -- **Orthostatic hypotension**
* Remedy: take drug at **bedtime**
Prazosins, Doxazosins, Terazosins
234
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
**ALPHA 1 SELECTIVE BLOCKERS**:
* used for **BPH** (enlargement of prostate)
* **obstructed urine passage** leading to significant **urine retention**
Finasteride, Dutasteride
235
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
**ALPHA 1 SELECTIVE BLOCKER**:
* **symptomatic relief** of urine retention
Tamsulosin, Alfuzosin
236
# **SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS**
ALPHA 2 BLOCKERS
Yohimbine
Rauwolscine
237
* **beta 1 antagonism**, mostly in the **heart**
* decrease **ionotropy**, **chronotropy**, **dromotropy**
* **cardiac depression**
BETA BLOCKERS
(-lol, -olol)
238
# **BETA BLOCKERS**
block beta 1, beta 2
NONSELECTIVE BETA BLOCKER
239
# **BETA BLOCKERS**
there is NO selective beta ____ blocker
beta 2
240
# **BETA BLOCKERS**
**beta 2** blockade
bronchoconstriction
241
# **BETA BLOCKERS**
Nadolol
Sotalol
Timolol
Propranolol
**Cart**eolol
**Carve**dilol
Labetalol
Penbutolol
Pindolol
NONSELECTIVE BETA BLOCKER
242
# **BETA BLOCKERS | NONSELECTIVE**
beta blockers are what class in **general**
class II
243
# **BETA BLOCKERS | NONSELECTIVE**
the ONLY **class III** beta blocker
anti **arrhythmic**
SOTALOL
244
# **BETA BLOCKERS | NONSELECTIVE**
how many classes of beta blockers
4 classes
245
# **BETA BLOCKERS | NONSELECTIVE**
Class I
Na channel
246
# **BETA BLOCKERS | NONSELECTIVE**
Class II
Beta channel
247
# **BETA BLOCKERS | NONSELECTIVE**
Class III
K channel
248
# **BETA BLOCKERS | NONSELECTIVE**
Class IV
Ca channel
249
# **BETA BLOCKERS | NONSELECTIVE**
anti**glaucoma**
Timolol
250
# **BETA BLOCKERS | NONSELECTIVE**
prototype with brand **Inderal**
Propranolol
251
# **BETA BLOCKERS**
Celiprolol
Bisoprolol
Betaxolol
Esmolol
Acebutolol, Atenolol
Metoprolol
Nebivolol
BETA 1 SELECTIVE - CARDIO SELECTIVE
252
# **BETA BLOCKERS | ADDITONAL MOA**
* **beta 2 agonist**
* Carteolol, Celiprolol
* Labetalol
* Acetabulol
* Pindolol, Penbutolo
INTRINSIC SYMPATHOMIMETIC ACTIVITY (ISA)
253
# **BETA BLOCKERS | ADDITONAL MOA**
INTRINSIC SYMPATHOMIMETIC ACTIVITY (ISA)
CLAP
Carteolol, Celiprolol
Labetolol
Acetabulol
Penbutolol, Pindolol
254
# **BETA BLOCKERS | ADDITONAL MOA**
* **local anesthesia**
* display risk in the **eyes**: **corneal injury**
* Propanolol, Pindolol
* Acetabulol
* Labetalol
* Metoprolol
MEMBRANE STABILIZERS
255
# **BETA BLOCKERS | ADDITONAL MOA**
MEMBRANE STABILIZERS
PALM
Pindolol, Propranolol
Acetabutolol
Labetalol
Metopolol
256
# **BETA BLOCKERS | ADDITONAL MOA**
VASODILATION:
through **alpha 1 blockade**
Carvedilol, Labetalol
257
# **BETA BLOCKERS | ADDITONAL MOA**
VASODILATION:
enhance **nitric oxide** level
MOST **CARDIOSELECTIVE**
Nevibolol
258
# **BETA BLOCKERS | USES**
1st line agent for **HTN** patient with history of ____
MYOCARDIAL INFARCTION
259
# **BETA BLOCKERS | USES**
management of ____
angina pectoris
stable heart failure - by blocking renin
260
# **BETA BLOCKERS | USES**
drugs used for management of **STABLE heart failure**
Bisoprolol
Carvedilol
Metoprolol **succinate**
Nebivolol
261
# **BETA BLOCKERS | USES**
management of ____ EXCEPT **Sotalol**
arrhythmia
262
# **BETA BLOCKERS | USES**
for **eye disorders**
Timolol
Betaxolol
263
# **BETA BLOCKERS | USES**
ENDOCRINE D/O:
tx of sympathetic symptom of **hyperthyroidism** such as **tachycardia** -- they inhibit **peripheral conversion** of T4 to T3
Propranolol
Carvedilol
264
# **BETA BLOCKERS | USES**
ENDOCRINE D/O:
**can** be sedating
Propranolol
265
# **BETA BLOCKERS | USES**
ENDOCRINE D/O:
**less** sedating
Carvedilol
266
problem with **hyperthyroidism**
high levels of T3
267
# **BETA BLOCKERS | USES**
* prophylaxis of **migraine**
* tx of **stage fright**
* symptomatic treatment of **alcohol withdrawal**
* used in **infantile hemangiomas** (birthmark)
PROPRANOLOL
268
# **BETA BLOCKERS**
TOXIC EFFECTS
* **bradycardia**
* mask **hypoglycemic symptom** (tachycardia)
* broncho**constriction**
* **hyper**lipidemia (by blocking b3)
269
MAIN NT of **Parasympathetic** drugs
ACETYLCHOLINE
270
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
BIOSYNTHESIS:
**active uptake** of ____
choline
271
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
BIOSYNTHESIS:
**choline entry** in ____
presynapse
272
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
BIOSYNTHESIS:
**rate limiting step**
active uptake of choline
273
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
BIOSYNTHESIS:
**transporter**
choline transporter
274
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
BIOSYNTHESIS:
**choline transporter inhibitor**
Hemicholinium
275
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
FORMATION:
combine with ____ from mitochondrion
acetyl CoA
276
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
FORMATION:
**catalyzing enzyme**
choline acetyl transferase
277
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
STORAGE:
entry to vesicles through ____
VAT: vesicle associated transporter
278
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
STORAGE:
**VAT inhibitor**
Vesamicol
279
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
RELEASE:
**exocytosis enhancer**
a-latrotoxin
280
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
RELEASER:
**exocytosis inhibitor**
botulinumtoxin
281
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
TERMINATION:
**enzyme for metabolism**
acetylcholinesterase
282
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
TERMINATION:
**hydrolyze Ach** to chloine and acetate
AChE
283
# **PARASYMPATHETIC DRUGS | ACETYLCHOLINE**
TERMINATION:
**AChE is inhibited by**
anticholinesterase
284
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | MUSCARINIC**
* in the **parietal cell**
* **activate** proton pump --> HCl production
* **ACIDITY**
M1
285
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | MUSCARINIC**
* in the **atria** of the heart
* **bradycaria**
M2
286
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | MUSCARINIC**
* in **exocrine glands** --> **wetness**: salivation, lacrimation, sweating
* in **smooth muscles** --> **contraction**
* EYES: ciliary --> **near vision**; circular muscles (in **iris**) --> **miosis**
* BRONCHI: broncho**constriction**
* GIT: **bowel movement**
* URINARY BLADDER: **urination**
M3
287
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC**
* **ganglion** --> synaptic neurotransmission
* **adrenal medulla** --> EPI release
NICOTINIC Neural (N)
288
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC**
NICOTINIC NEURAL:
**synaptic neurotransmission**
ganglion
289
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC**
NICOTINIC NEURAL:
**EPI release**
adrenal medulla
290
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC**
* **neuromuscular end plates** --> skeletal muscle contraction
NICOTINIC MUSCULAR (M)
291
# **PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC**
NICOTINIC MUSCULAR:
**skeletal muscle contraction**
neuromuscular end plates
292
# **PARASYMPATHETIC DRUGS**
AGONIST
Cholinomimetics
293
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS**
* cholinoceptor **activation**: drug **binding**
DIRECT ACTING
294
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
CHOLINE ESTERS:
* ACTIVATE **muscarinic** and **nicotinic** receptor
* Acetylcholine
* Carbachol
* Methacholine
NONSELECTIVE
295
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
CHOLINE ESTERS:
**NONSELECTIVE**
Acetylcholine
Carbachol
Metacholine
| ACM
296
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
CHOLINE ESTERS | **NONSELECTIVE**:
* broncho**constrictor**
* diagnostic agent in patient with suspected **bronchial asthma**: pulmonary challenge test
Methacholine
297
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
CHOLINE ESTERS:
* **Bethanechol** (Urecholine)
MUSCARINIC SELECTIVE
298
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
CHOLINE ESTERS | **MUSCARINIC SELECTIVE**:
* management in the tx of **urine retention**
Bethanechol (Urecholine)
299
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
ALKALOIDS:
**nonselective**
Arecoline
300
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
ALKALOIDS:
**muscarinic selective**
Muscarine
Pilocarpine
301
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
ALKALOIDS | **MUSCARINIC SELECTIVE**:
* for mgt of **glaucoma**
* for mgt of **GI atony** (no contraction)
PILOCARPINE
302
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
ALKALOIDS:
* for mgt of **smoking cessation**
* Nicotine
* Lobeline
* Varenicline
NICOTINIC SELECTIVE
303
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING**
ALAKLOIDS | **NICOTINIC SELECTIVE**:
* NOT FDA approved
Lobeline
304
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS**
* **inhibit** Ach metabolism = **enhance** ACh for action
* aka **anticholinesterase**
INDIRECT acting
305
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
* **SAFE**
* Aminoalcohol
* Carbamates
REVERSIBLE
306
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
REVERSIBLE:
**aminoalcohol**
Edrophonium (Tensilon)
307
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
REVERSIBLE:
**carbamates**
Physo**stigmine**/Eserine
Pyrido**stigmine**
Neo**stigmine**
Ambenon**ium**
Demecar**ium**
308
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
REVERSIBLE | **CARBAMATES**:
BRAND NAME of **Physostigmine**
Eserine
309
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
ORGANOPHOSPHATES
IRREVERSIBLE
310
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
IRREVERSIBLE:
**Agricultural poision (Insecticides)**
Malathion, Parathion
311
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
IRREVERSIBLE:
**nerve gases**
Soman
Tabbun
Sarin
312
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
IRREVERSIBLE:
ONLY **clinically useful**
Echothiophate
313
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING**
Tacrine
Donepezil
Galantamine
Rivastigmine
CNS acting
314
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
management for ____
alzheimer's disease
myasthenia gravis
315
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ALZHEIMER'S DISEASE:
* **abnormal protein fragments** (beta-amyloid) accumulate between nerve cells, **disrupting communication** and **triggering inflammation**
BETA AMYLOID PLAQUES
316
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ALZHEIMER'S DISEASE:
* **Tau protein** inside neurons becomes defective, **forming tangles** that **block nutrient transport**, leading to **cell death**
NEUROFIBRILLARY TANGLES
317
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ALZHEIMER'S DISEASE:
* **progressive loss** of neurons, particularly in the **hippocampus** and **cortex**, results in **memory loss** and **cognitive decline**
NEURONAL DAMAGE & BRAIN SHRINKAGE
318
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ALZHEIMER'S DISEASE:
**general effect**
low Ach
319
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ALZHEIMER'S DISEASE:
**treatment**
CNS acting cholinergics --> increase ACh effects
320
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
* a neuromuscular disease leading to **fluctuating muscle weakness** and **fatiguability** --> progressive muscle weakness
* an **autoimmune disorder** ibn which **weakness** is caused by **circulating antibodies** that **block acetylcholine receptors** at the **post-synaptic neuromuscular junction**
* SYMPTOM: **Ptosis** of the **left eye** (drooping eyelids)
* DIAGNOSIS: **Edrophonium** (Tensilon test)
* TREATMENT: **Carbamates**
MYASTHENIA GRAVIS
321
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
MYASTHENIA GRAVIS:
**symptom**
ptosis of the left eye
(drooping eyelids)
322
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
MYASTHENIA GRAVIS:
**diagnosis**
Edrophonium (Tensilon test(
323
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
MYASTHENIA GRAVIS:
**treatment**
carbamates
324
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
management for **glaucoma**; **lower IOP**
Echothiophate
Demecarium
325
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
GI atony
Physostigmine
326
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ANTIDOTES:
* for **Atropine** poisoning
* can enter the brain **targeting both central & peripheral**
PHYSOSTIGMINE
327
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ANTIDOTES:
* for **other anticholinergic** poisoning
NEOSTIGMINE
328
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE**
ANTIDOTES:
* for **NMB toxicity**
Edrophonium + Neostigmine
329
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT**
TOXIC EFFECTS
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation salivation, sweating
330
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT**
TREATMENT FOR TOXIC EFFECTS:
**Early (short)**
cholinesterase activators
Pralidoxime
Diacetylmonoxime
331
# **PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT**
TREATMENT FOR TOXIC EFFECTS:
**Late (long)**
anticholinergic
Atropine
332
# **PARASYMPATHETIC DRUGS**
ANTAGONISTS
CHOLINOLYTICS
333
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS**
ANTI**MUSCARINIC**/ANTI**CHOLINERGIC**:
prototype
ATROPINE
334
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
pharmacologic effects of ATROPINE
sympathetic effect
335
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS:
**M1 blockade**
inhibit HCl production
336
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS:
**M2 blockade**
tachycardia
337
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS | **M3 blockade**:
EXOCRINE GLANDS
DRYNESS - xerostomia, anhidrosis, hyperthermia, erythema
338
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS | **M3 blockade**:
SMOOTH MUSCLES
relaxation
339
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS | **M3 blockade**:
EYES: **ciliary**
cycloplegia
340
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS | **M3 blockade**:
EYES: **muscles**
mydriasis
341
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS | **M3 blockade**:
**bronchi**
bronchodilation
342
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS | **M3 blockade**:
**GIT**
ileus
343
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
PERIPHERAL EFFECTS **M3 blockade**:
**urinary bladder**
retention
344
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
* tx for **symptomatic BRADYCARDIA**
* tx of **CHOLINOMIMETIC poisoning**
* given with **diphenoxylate** as **antidiarrheal**
* **adjunct** treatment for **parkinsonism**
* anti**spasmodic**
ATROPINE
345
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
ATROPINE is given with ____ as anti**diarrheal** to **lessen addiciton**
diphenoxylate
346
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
CNS ACTING:
* mgt of **extrapyrimidal syndrome** (SE of antipsychotics)
* mgt of **parkinsonism**
Benztropine
Biperiden
Trihexyphenidyl
| BBT
347
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
CNS ACTING:
* used in the tx of **motion sickness**
scopalamine
348
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
EYE ACTING:
* for **eye exam**
Mydriatics
349
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
EYE ACTING:
* tx of **pain** during **eye injury**
* Homatropine
* Anistropine
* Cyclopentolate
Cyloplegics
350
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
**bronchi acting** cholinergics causes
relaxation (dilation)
351
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
BRONCHI ACTING:
**SHORT** acting muscarinic antagonist (SAMA)
**Ipra**tropium
**Oxy**tropium
352
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
BRONCHI ACTING:
**LONG** acting muscarinic antagonist (LAMA)
**Tio**tropium
353
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
GASTRIC GLAND ACTING:
* mgt of **hyperacidity**
**Piren**zepine
**Telen**zepine
354
# **PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG**
GIT & URINARY BLADDER ACTING:
* for mgt of **urine incontinence**, **hypermotility**
Methscopalamine
Glycopyrolate
HNBB
Dicycloverine
Oxybutinin
Scopalamine
355
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC**
* **Ganglionic** blockers
* **obsolete** antihypertensive
* **Hexamethonium**, **Trimethaphan**, **Mecamylamine**
NN blockers
356
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC**
NN blockers
Hexamethonium
Trimethaphan
Mecamylamine
357
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC**
* **skeletal muscle relaxants**
* used as **anesthetic adjunt** to **relax skeletal muscles** prior surgery
* tx of **spastic disorders** such as **spastic cerebral palsy**
* to facilitate **endotracheal intubation**
* in **tetanus** to **reduce muscle spasms**
NM blockers
358
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS**
MOA: **irreversible** NM receptor activation producing
* INITIAL effect: **depolarization** and **overstimulation** of NM receptor
* FINAL effect: **desensitization** = **relaxation**
DEPOLARIZING / IRREVERSIBLE / NONCOMPETITIVE
359
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS**
DEPOLARIZING / IRREVERSIBLE / NONCOMPETITIVE:
**INITIAL** effect
depolarization & overstimulation of NM receptor
360
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS**
DEPOLARIZING / IRREVERSIBLE / NONCOMPETITIVE:
**INITIAL**: agonist binds to the receptor causing depolarization of the membrane and will result to **initial discharge** causing ____ followed by **flaccid paralysis**
fasciculations
361
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS**
DEPOLARIZATION / IRREVERSIBLE / NONCOMPETITIVE:
* **slow** dissociation of the agonist
* agonist **remains bound** to the receptor
* membrane **repolarizes** but **receptor is desensitized** to the effect of ACh
FINAL EFFECT
362
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING**
* **MOST PREFERRED**
* duration of action is **extremely short** since it is rapidly degraded by **plasma cholinesterase**
* DOA: **3-5mins**, given by **IV infusion**
* **less likely** to cause toxicity -- paralyzing effect on respiratory muscle **easil wears off** upon termination of the infusion
* preferred in **surgical anesthesia**
SUCCINYLCHOLINE
363
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING**
SUCCINYLCHOLINE:
DOA
3-5 mins
364
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING**
SUCCINYLCHOLINE:
given by
IV infusion
365
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING**
SUCCINYLCHOLINE:
**order of paralysis**
1. Fasciculations in chest & abdomen
2. Neck, arms, legs
3. Facial, pharynx, larynx
4. Respiratory muscles
366
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING**
**TOO LONG** duration of action
Decamethonium
367
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING**
Action is **shorter** than decamethonium since it is **rapidly metabolized** by **cholinesterase**
Suxamethonium
368
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS**
* **SAFER**
* with ACh at the nicotinic receptors at the neuromuscular junction
* **NO muscle contraction**
* **curare** derivatives
* MOA: block NM receptors = **immediate relaxation** = **paralysis**
NONDEPOLARIZING / REVERSIBLE / COMPETITIVE
| **antagonist**
369
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | NONDEPOLARIZING**
ISOQUINOLINE
curium
370
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | NONDEPOLARIZING**
STEROIDAL
curonium
371
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS**
GENERAL
skin wheals
transient hypotension
tachy brady
respiratory/diaphragmatic paralysis
372
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS**
SUCCINYLCHOLINE
myalgia, myositis
rhabdomyolysis
malignant hypothermia
373
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS**
TUBOCURARINE
increase degranulation leading to **anaphylactoid** reaction
374
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS**
TUBOCURARINE TOXICITY:
**treatment**
Epinephrine
375
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | REVERSAL**
* increasing the **availability** of **ACh** at the motor end plate, mainly by **inhibition** of **acetylcholinesterase**
* to a **lesser extent**, these cholinesterase inhibitors also **increase** the **release** of this transmitter from the motor nerve terminal
NEOSTIGMINE & PYRIDOSTIGMINE
376
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | REVERSAL**
* **antagonizes NEUROMUSCULAR BLOCKADE** purely by **inhibiting acetylcholinesterase activity**
EDROPHONIUM
377
# **PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | REVERSAL**
* for **RAPID REVERSAL** of the steroid neuromuscular blocking agents -- ***rocuronium & vecuronium***
* binds ti plasma rocuronium to **decrease** its **free plasma concentration** and **diffuse away** from the neuromuscular junction
SUGAMMADEX
