M4 Flashcards
VOLUNTARY control of skeletal muscle
SOMATIC NS
INVOLUNTARY control of glands and smooth muscle
AUTONOMIC NS
AUTONOMIC NS
FIGHT OR FLIGHT
SYMPATHETIC
AUTONOMIC NS
REST AND DIGEST
PARASYMPATHETIC
- 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)
AUTONOMIC NERVOUS SYSTEM
AUTONOMIC NS
subdivision of the ____ nervous system
peripheral effector
AUTONOMIC NS
composed of ____ neuron that connect the brain and effector organ
2 motor neurons
AUTONOMIC NS
usually controls the activity of the organs covered by a ____
viscera
- explain the mechanism of impulse transport across the synapse
- presence of gaps or spaces
- nervous system is discontinuous
SYNAPTIC NEUROTRANSMISSION
SYNAPTIC NEUROTRANSMISSION
explain the mechanism of ____ across the synapse
impulse transport
SYNAPTIC NEUROTRANSMISSION
presence of gaps and spaces
synapse
SYNAPTIC NEUROTRANSMISSION
nervous system is ____
discontinuous
the region BETWEEN pre ganglion and post ganglion
ganglion
SYNAPTIC NEUROTRANSMISSION
- synthesis, storage (vesicles), release or exocytosis of NT
- has enzymes: metabolism
- has autoreceptors: inhibitory effect
PRESYNAPSE
SYNAPTIC NEUROTRANSMISSION
PRESYNAPSE:
auto receptors: ____ effect
inhibitory
SYNAPTIC NEUROTRANSMISSION
parts of synapse
presynapse
cleft
post synapse
SYNAPTIC NEUROTRANSMISSION
has enzymes: metabolism
cleft
SYNAPTIC NEUROTRANSMISSION
- has the majority of receptors: excitatory effect
- enzymes: metabolism
POST SYNAPSE
SYNAPTIC NEUROTRANSMISSION
POST SYNAPSE:
majority of receptors: ____ effect
excitatory
SYNAPTIC NEUROTRANSMISSION
induces release or exocytosis
Calcium ion
SUBDIVISION OF ANS
bronchioles of the lungs:
DILATION
SYMPATHETIC
SUBDIVISION OF ANS
bronchioles of the lungs:
CONSTRCITION
PARASYMPHATETIC
SUBDIVISION OF ANS
secretion of adrenaline and NA
SYMPATHETIC
SUBDIVISION OF ANS
salivation
PARASYMPATHETIC
SUBDIVISION OF ANS
____ responses dominate when the person is under STRESS, EXERCISE, or IN MOTION (such as running)
SYMPATHETIC
SUBDIVISION OF ANS
____ dominates when the person is AT REST (energy is conserved); during sleep
PARASYMPATHETIC
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
ORIGIN OF NEURONS:
sympathetic
T1-T12; L1-L5
Thoracolumbar NS
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
ORIGIN OF NEURONS:
parasympathetic
CN 3,7,9,10; S2-S4
Craniosacral NS
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
LENGTH OF NEURONS:
sympathetic
SHORT pre ganglion
LONG post ganglion
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
LENGTH OF NEURONS:
parasympathetic
LONG pre ganglion
SHORT post ganglion
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
LOCATION OF GANGLION:
sympathetic
near spinal cord
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
LOCATION OF GANGLION:
parasympathetic
near effector organ
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
sympathetic
PRE ganglion
ACETYLCHOLINE
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
sympathetic
POST ganglion
NOREPINEPHRINE
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
parasympathetic
PRE ganglion
Acetylcholine
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
SYNTHESIS, STORAGE, & RELEASE OF NT (PRESYNAPSE):
parasympathetic
POST ganglion
Acetylcholine
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
MAJOR/PRIMARY NT of PARASYMPATHETIC
Acetylcholine
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
MAJOR/PRIMARY NT of SYMPATHETIC
NOREPINEPHRINE
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
RECEPTORS (POST SYNAPSE):
sympathetic
GANGLION
NICOTINIC NEURAL
(QISS)
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
RECEPTORS (POST SYNAPSE):
sympathetic
EFFECTOR
ADRENORECEPTORS
(a-1, b-1,2)
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
RECEPTORS (POST SYNAPSE):
parasympathetic
GANGLION
NICOTINIC NEURAL
(QIQ)
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
RECEPTORS (POST SYNAPSE):
parasympathetic
EFFECTOR
CHOLINORECEPTORS: muscarinic, nicotinic
SYMPATHETIC VS PARASYMPATHETIC | ANATOMICAL DIFFERENCES
PARA | EFFECTOR:
nicotinic binds to ____
sodium channel
SYMPATHETIC VS PARASYMPATHETIC
- sweat glands
more PRIMARILY parasympathetic but may part na sympathetic
SYMPATHETIC VS PARASYMPATHETIC
cardiac and smooth muscle, gland cells, nerve terminals
PARA & SYMPA
SYMPATHETIC VS PARASYMPATHETIC
renal vascular smooth muscle
SYMPATHETIC
SYMPATHETIC VS PARASYMPATHETIC
skeletal muscle
SOMATIC
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
response related to stress
FIGHT OR FLIGHT
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
response during basal conditions
rest and digest
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
NE vs Ach
functional antagonist
(different targets, opposite effects)
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
heart
tachycardia
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
heart
bradycardia
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
pupils
mydriasis
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
NE
Adrenergic nervous system
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
ACh
Cholinergic Nervous system
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
pupils
miosis
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
bronchi
bronchodilation
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
bronchi
bronchoconstriction
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
GIT
ILEUS: loss of peristalsis
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPHATETIC:
GIT
bowel movement
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
urinary bladder
urine retention
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
urinary bladder
urination
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
SYMPATHETIC:
sweating
APOCRINE: palms & soles
SYMPATHETIC VS PARASYMPATHETIC | FUNCTIONAL DIFFERENCE
PARASYMPATHETIC:
sweating
ECCRINE: generalized for thermoregulation
- 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
ENTERIC NERVOUS SYSTEM
considered a ____ of ANS
3rd division
ENTERIC NERVOUS SYSTEM
located in the
walls of GI system
ENTERIC NERVOUS SYSTEM
includes ____ and ____
Myenteric Plexus
Submucous Plexus
ENTERIC NERVOUS SYSTEM
PARASYMPATHETIC
activates ENS
ENTERIC NERVOUS SYSTEM
SYMPATHETIC
inhibits ENS
ENTERIC NERVOUS SYSTEM
Myenteric Plexus is also known as
Auerbach’s Plexus
ENTERIC NERVOUS SYSTEM
Submucous Plexus is also known as
Meissner’s Plexus
ENTERIC NERVOUS SYSTEM
MYENTERIC:
location
between the circular & longitudinal muscle layers of the gut wall
ENTERIC NERVOUS SYSTEM
SUBMUCOUS:
location
within the submucosa of the GI tract
ENTERIC NERVOUS SYSTEM
MYENTERIC:
function
controls GI motility (peristalsis) and muscle contractions
ENTERIC NERVOUS SYSTEM
SUBMUCOUS:
function
regulates secretions and blood flow in the intestinal mucosa
ENTERIC NERVOUS SYSTEM
MYENTERIC:
neuronal composition
contains motor neurons and interneurons controlling smooth muscle
ENTERIC NERVOUS SYSTEM
SUBMUCOUS:
neuronal composition
composed of sensory neurons and secretomotor neurons
ENTERIC NERVOUS SYSTEM
MYENTERIC:
influence
affects the entire GI tract, from the esophagus - rectum
ENTERIC NERVOUS SYSTEM
SUBMUCOUS:
influence
more prominent in the small and large intestines
ENTERIC NERVOUS SYSTEM
MYENTERIC:
effect on digestion
regulates movement of food through the gut
ENTERIC NERVOUS SYSTEM
SUBMUCOUS:
effect on digestion
modulates enzyme secretion and absorption processes
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- EXCITATORY neurotransmitter
- stimulates smooth muscle contraction, increases glandular secretions
ACETYLCHOLINE
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- INHIBITORY (mostly sympathetic influence)
- decreases motility and secretions, contracts sphincters
NOREPINEPHRINE
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- modulates GUT motility and secretion
- stimulates peristalsis, affects sensory neurons, and regulates secretion
SEROTONIN
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- modulates ENS neuronal activity
- inhibitis excessive motility, reduces Ach release
DOPAMINE
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- INHIBITORY neurotransmitter
- relaxes smooth muscles, promotes vasodilation
NITRIC OXIDE
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- regulates smooth muscles and secretions
- relaxes gut muscles, increases intestinal secretion, and dilation of blood vessels
VASOACTIVE INTESTINAL PEPTIDE (VIP)
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- EXCITATORY, involved in pain perception
- stimulates smooth muscle contraction, enhances pain signaling
SUBSTANCE P
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- MODULATE motility and pain perception
- INHIBIT peristalsis, REDUCE pain sensation
ENKEPHALINS (opioid peptides)
ENTERIC NERVOUS SYSTEM | TRANSMITTERS
- acts as a neurotransmitter in the ENS
- can INDUCE muslce relaxation and MODULATE ENS signaling
ATP (Adenosine Triphosphate)
SYMPATHETIC DRUGS
Major NT
NOREPINEPHRINE
SYMPATHETIC DRUGS
agonists
-mimetics
SYMPATHETIC DRUGS
antagonists
-lytics
SYMPATHETIC DRUGS
ENDOGENOUS catecholamines
Epinephrine,
Norepinephrine,
Dopamine
SYMPATHETIC DRUGS
ENDOGENOUS CATECHOLAMINES:
1st to be synthesized
Dopamine
SYMPATHETIC DRUGS
ENDOGENOUS CATECHOLAMINES:
2nd to be synthesized
Norepinephrine
SYMPATHETIC DRUGS
ENDOGENOUS CATECHOLAMINES:
3rd to be synthesized
Epinephrine
synthesize tyrosine to L-dopa
tyrosine hydroxylase
inhibits tyrosine hydrxylase
METYROSINE
inhibits storage of dopamine
Reserpine / Tetrabenazine
exocytosis inhibitor in the presynapse
Bretyllium, Guanethidine
reuptake inhibitor (presynapse)
Cocaine
Tricyclic antidepressants
SYMPATHETIC DRUGS
biosynthesis of endogenous catecholamine
Tyrosine -> L-dopa -> Dopamine -> Norepinephrine -> Epinephrine
SYMPATHETIC DRUGS
precursor to the conversion of L-dopa
tyrosine
SYMPATHETIC DRUGS
- the rate limiting enzyme in production of endogenous catecholamines
- inhibited by Metyrosine (decrease sympathetic effect)
TYROSINE HYDROXYLASE
SYMPATHETIC DRUGS
Formation of Dopamine:
enzyme
L-DOPA carboxylase
SYMPATHETIC DRUGS
Formation of NE occurs where
inside the vesicles
SYMPATHETIC DRUGS
Formation of NE:
enzyme
Dopamine-B-hydroxylase
SYMPATHETIC DRUGS
Formation of Epinephrine occurs in the ____
adrenal medulla
SYMPATHETIC DRUGS
Formation of Epinephrine:
enzyme
PENMT: Phenylethanolamine-N-methyltransferase
SYMPATHETIC DRUGS
PREVENT premature metabolism of dopamine
storage of dopamine
SYMPATHETIC DRUGS
STIMULANTS of exocytosis
greater for NE binding
Tyramine
Ephedrine
Amphetamine, Angiotensin II
Methamphenamine
TEAM
SYMPATHETIC DRUGS
INHIBITORS of exocytosis
less NE for binding
Guanethidine
Guanadrel
Bretylium
GGB
SYMPATHETIC DRUGS
TERMINATION occurs in the ____
cleft
SYMPATHETIC DRUGS
REDUCE NE for binding
Termination
SYMPATHETIC DRUGS
REUPTAKE inhibitors
increase NE for binding
Cocaine
Atomoxetine
Sibutramine
CAS
SYMPATHETIC DRUGS
enzymes for METABOLISM
Monoamine Oxidase (MAO)
Catechol-O-Methyltrasnferase (COMT)
SYMPATHETIC DRUGS
PRODUCTS of metabolism:
EPI, NE
3-methoxy-4-hydroxymandelic acid or VMA (vanillylmandelic acid)
SYMPATHETIC DRUGS
PRODUCTS of metabolism:
DOPAMINE
homovanillic acid
SYMPATHETIC DRUGS
MAO inhibitors
MPITS
SYMPATHETIC DRUGS
COMT inhibitors
-capones
SYMPATHETIC DRUGS | ADRENORECEPTORS
GPCRs
QISS Alpha receptors
Type 2 metabotropic receptors
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
smooth muscle
contraction
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
blood vessel
vascoconstriction
increase BP
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
bladder trigone, sphincter CLOSURE
urine retention
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
prostatic smooth muscle
contraction = urine retention
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
radial muscles (iris)
contraction = MYDRIASIS
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
sphincter muscle
contraction of iris
bigger pupils -> MIOSIS
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 1:
pilomotor smooth muscles (skin)
PILOERECTION (goosebumps)
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
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 2:
POST synaptic
Peripheral blood vessel (usually in the eyes)
VASOCONSTRICTION
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
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 2:
* helps manage opioid and nicotine withdrawal by decreasing sympathetic overactivity
Reduction of Opiate Withdrawal Symptoms
SYMPATHETIC DRUGS | ADRENORECEPTORS
ALPHA 2:
* some a2 agonists reduce aqueous humor production, lowering intraocular pressure in glaucoma
decreased Intraocular pressure
SYMPATHETIC DRUGS | ADRENORECEPTORS
- HEART = increase inotropy, chronotropy, dromotropy = cardiac stimulation
- KIDNEY = increase renin
BETA 1 receptor
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 1:
important for synthesis of angiotensin II = increase BP
RENIN
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 1:
* specific region with beta 1 receptor
* specific region where beta 1 are
JUXTAGLOMERULAR APPARATUS
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 2:
smooth muscles
relaxation
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 2:
bronchi
bronchodilation
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 2:
uterus
tocolysis
(relaxation of uterus)
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 2:
blood vessels (skeletal muscles)
vasodilation
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 2:
skeletal muscles contraction
tremors
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 2:
skeletal muscle ____ iptake in the muscles = hypokalemia
enhance K ion uptake
low levels of K ion in the blood leads to hypokalemia
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 3:
fat cells
adipocytes
SYMPATHETIC DRUGS | ADRENORECEPTORS
BETA 3:
break down of fats
lipolysis
weight loss
SYMPATHETIC DRUGS | ADRENORECEPTORS
activation of BETA 3 leads to
lipolysis
SYMPATHETIC DRUGS
agonists
SYMPATHOMIMETICS
SYMPATHETIC DRUGS | SYMPATHOMIMETICS
adrenoceptor activation: drug binding to receptor
DIRECT acting sympathomimetics
SYMPATHETIC DRUGS | SYMPATHOMIMETICS
- enhance level of NE for binding
- enhance exocytosis
- inhibit reuptake
INDIRECT acting sympathomimetics
SYMPATHETIC DRUGS | SYMPATHOMIMETICS
direct + indirect
enhance exocytosis
MIXED ACTING sympathomimetics
SYMPATHETIC DRUGS | SYMPATHOMIMETICS
- Nonselective
- Selective
Direct acting
SYMPATHETIC DRUGS | SYMPATHOMIMETICS
DIRECT ACTING:
* activate MORE THAN 1 sympathetic receptor (alpha and beta)
* endogenous catecholamines: EPI, NE, DA
NONSELECTIVE
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
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
high POTENCY at ____
adrenoreceptors
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
higher AFFINITY in ____ than ____
in beta than alpha
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
BETA effect at ____ dose
LOW
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
ALPHA effect at
____ dose
HIGH
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE DIRECT ACTING
EPI, NE, DA
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
* the ONLY bronchodilating
* B1 = B2»_space;> a1
* the ONLY that has activity at B2 = only bronchodilating endogenous
EPINEPHRINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
B1 > a1
NOREPINEPHRINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
D1 > B1»_space; a1
DOPAMINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
* enhance renal vasodilation
* increase GFR
* increase diuresis
D1
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
____ BBB
Polar/Hydrophilic
Impermeable - cannot pass
NO CNS effects
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
extensively metabolized by
MAO and COMT
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
duration of action
SHORT
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
oral bioavailability
LOW
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
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
1ST LINE for
cardiac stimulant
tx of anaphylactic shock
anaphylaxis
anaphylactoid
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
* increase histamine = bronchoconstriction
* IgE mediated
anaphylaxis
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
* increase histamine = bronchoconstriction
* NON IgE mediated; drug induced
* can be caused by: Morphine, Tubocurarine, Guanethedine
anaphylactoid
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | EPINEPHRINE/ADRENALINE:
local vasoconstrictor combined with ____
LIDOCAINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | EPI/ADRENALINE:
* for GLAUCOMA
* prodrug of EPI
* pivalic acid ester of EPI
DIPIVEFRIN
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE:
1ST LINE for SEPTIC SHOCK (caused by infection)
NOREPINEPHRINE / NORADRENALINE / LEVARTERENOL
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
LOW urine output
oliguria & anuria
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | TOXIC EFFECTS:
a1 overstimulation = vascoconstriction
HTN, digital necrosis (purple fingers, poisoning)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | TOXIC EFFECTS:
b1 overstimulation
ventricular tachycardia
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE | TOXIC EFFECTS:
treatment for b1 overstimulation = VENTRICULAR TACHYCARDIA
PHENTOLAMINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE:
* CONSTRICTOR drugs
* Phenylephrine, Methoxamine
* Propylhexedrine
* Tetrahydrozoline, Oxymetazoline, Nafazoline
ALPHA1 AGONIST
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE:
Alpha 1 agonist
Phenylephrine, Methoxamine
Propylhexedrine
Tetrahydrozoline, Oxymetazoline, Nafazoline
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
effects
vasoconstriction
mydriasis
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
local effects
intrasal
eye drops
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
nasal spray - decongestant
Oxymetazoline (Drixine)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
eye drops - treatment of red eyes
Tetrahydroziline (Eye Mo Red)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
systemic effects
for nasal congestion
tx of hypotension
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
MYDRIATIC in eye examination = for full view of retina
PHENYLEPHRINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
LOCAL toxic effect
rhinitis medicamentosa
rebound congestion if used more than 3 days
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 1 AGONIST:
SYSTEMIC toxic effects
- increase blood pressure
- urine retention
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE:
* antiglaucoma agents: Apraclonidine, Brimonidine
* antihypertensive agents: Methyldopa, Clonidine, Guanfacine, Guanabenz
ALPHA 2 AGONIST
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
antiglaucoma agents
Apraclonidine, Brimonidine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
antihypertensive agents
Methyldopa, Clonidine, Guanfacine, Guanabenz
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
BRAND NAME methyldopa
Aldomet
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
BRAND NAME Clonidine
Catapres
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
* PRODRUG of methyldopa
* a FALSE NT
a-methyl-norepinephrine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
MOA of Clonidine
Initial: increase BP
Final: decrease BP
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
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
CLINICAL USE Clonidine
HTN crisis
(general increase in BP)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
TOXIC EFFECTS methyldopa
Sedation
Hepatotoxicity
positive Coombs test
positive Hemolytic anemia
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
SELECTIVE | ALPHA 2 AGONIST:
TOXIC EFFECTS Clonidine
Withdrawal
Rebound HTN
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
NONSELECTIVE BETA AGONIST:
* alternative agent during shock
* alternative in the management of acute heart failure
Isoproterenol / Isoprenaline
na shock si TERE PRE! nagka heart failure
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
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
SHORT ACTING
Terbutaline
Albuterol
Metaprotrenol
Pirbuterol
TAMP
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
LONG ACTING
Salmeterol
Formoterol
Indacaterol
Bambuterol
SFIB
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
short acting that is the ONLY subcutaneous
Terbutaline
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
brand name of Albuterol
Salbutamol
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
long acting that has SLOW onset
Salmeterol
mabagal si SALM
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
long acting that has FAST onset
Formoterol
mabilis ang MOTER (motor)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
CLASSES
SABA
LABA
Tocolytics
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
the ONLY oral LONG ACTING
Bambuterol
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
* treatment of preterm labor
* relax uterine smooth muscle
TOCOLYTICS
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
TOCOLYTICS
Isoxsuprine (Duvadilan)
Ritodrine
Terbutaline
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
OFF LABEL tocolytic
Terbutaline
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | DIRECT ACTING
BETA 2 SELECTIVE AGONIST:
TOXIC EFFECTS
- Hyppokalemia
- Ventricular tachycardia (due to overdose – can activate BETA 1)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
* has D/I with MAOI = increase NE = hypertensive crisis
TYRAMINE
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
* from Ma Huang
Ephedrine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
* alternative for ADHD
Amphetamine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS
Tyramine
Ephedrine
Amphetamine
Metamphetamine
Modafinil
Methylphenidate
Phenmetrazine
TEAM MMP
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
shabu
Methamphetamine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
1st line agent for narcolepsy
Modafinil
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
1st line agent for ADHD
Methylphenidate
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
RELEASERS:
anorexiant
Phenmetrazine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
REUPTAKE INHIBITORS:
ONLY vasoconstrictor local anesthetic
Cocaine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
REUPTAKE INHIBITORS
Cocaine
Atomoxetine
Sibutramine
CAS
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
REUPTAKE INHIBITORS:
alternative agent for ADHD
Atomoxetine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
REUPTAKE INHIBITORS:
used in management of obesity, discontinued in the Philippines due to unnecessary cardiovascular risks to patients
Sibutramine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
APPETITE SUPPRESSANT:
typically prescribed for SHORT-TERM weight loss
Phentermine
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
APPETITE SUPPRESSANT:
a FAT ABSORPTION inhibitor that helps with weight management
Orlistat (Xenical, Alli)
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | INDIRECT ACTING
APPETITE SUPPRESSANT:
an injectable medication that regulates appetite and caloric intake
Liraglutide (Saxenda)
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)
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
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | MIXED ACTING
why is Phenylpropanolamine removed from the market
due to hemorrhagic stroke in young women
SYMPATHETIC DRUGS | SYMPATHOMIMETICS | MIXED ACTING
used for hypotension
Mephentermine
Metaraminol
SYMPATHETIC DRUGS
ANTAGONISTS
SYMPATHOLYTICS
SYMPATHETIC DRUGS
effect of SYMPATHOLYTICS
Parasympathetic effects
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
1st line agent for Carcinoid syndrome / Serotonin syndrome
Cyproheptadine
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
SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS
-zosins
ALPHA 1 SELECTIVE BLOCKERS
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
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
SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS
ALPHA 1 SELECTIVE BLOCKER:
* symptomatic relief of urine retention
Tamsulosin, Alfuzosin
SYMPATHETIC DRUGS | SYMPATHOLYTICS | NONSELECTIVE ALPHA BLOCKERS
ALPHA 2 BLOCKERS
Yohimbine
Rauwolscine
- beta 1 antagonism, mostly in the heart
- decrease ionotropy, chronotropy, dromotropy
- cardiac depression
BETA BLOCKERS
(-lol, -olol)
BETA BLOCKERS
block beta 1, beta 2
NONSELECTIVE BETA BLOCKER
BETA BLOCKERS
there is NO selective beta ____ blocker
beta 2
BETA BLOCKERS
beta 2 blockade
bronchoconstriction
BETA BLOCKERS
Nadolol
Sotalol
Timolol
Propranolol
Carteolol
Carvedilol
Labetalol
Penbutolol
Pindolol
NONSELECTIVE BETA BLOCKER
BETA BLOCKERS | NONSELECTIVE
beta blockers are what class in general
class II
BETA BLOCKERS | NONSELECTIVE
the ONLY class III beta blocker
anti arrhythmic
SOTALOL
BETA BLOCKERS | NONSELECTIVE
how many classes of beta blockers
4 classes
BETA BLOCKERS | NONSELECTIVE
Class I
Na channel
BETA BLOCKERS | NONSELECTIVE
Class II
Beta channel
BETA BLOCKERS | NONSELECTIVE
Class III
K channel
BETA BLOCKERS | NONSELECTIVE
Class IV
Ca channel
BETA BLOCKERS | NONSELECTIVE
antiglaucoma
Timolol
BETA BLOCKERS | NONSELECTIVE
prototype with brand Inderal
Propranolol
BETA BLOCKERS
Celiprolol
Bisoprolol
Betaxolol
Esmolol
Acebutolol, Atenolol
Metoprolol
Nebivolol
BETA 1 SELECTIVE - CARDIO SELECTIVE
BETA BLOCKERS | ADDITONAL MOA
- beta 2 agonist
- Carteolol, Celiprolol
- Labetalol
- Acetabulol
- Pindolol, Penbutolo
INTRINSIC SYMPATHOMIMETIC ACTIVITY (ISA)
BETA BLOCKERS | ADDITONAL MOA
INTRINSIC SYMPATHOMIMETIC ACTIVITY (ISA)
CLAP
Carteolol, Celiprolol
Labetolol
Acetabulol
Penbutolol, Pindolol
BETA BLOCKERS | ADDITONAL MOA
- local anesthesia
- display risk in the eyes: corneal injury
- Propanolol, Pindolol
- Acetabulol
- Labetalol
- Metoprolol
MEMBRANE STABILIZERS
BETA BLOCKERS | ADDITONAL MOA
MEMBRANE STABILIZERS
PALM
Pindolol, Propranolol
Acetabutolol
Labetalol
Metopolol
BETA BLOCKERS | ADDITONAL MOA
VASODILATION:
through alpha 1 blockade
Carvedilol, Labetalol
BETA BLOCKERS | ADDITONAL MOA
VASODILATION:
enhance nitric oxide level
MOST CARDIOSELECTIVE
Nevibolol
BETA BLOCKERS | USES
1st line agent for HTN patient with history of ____
MYOCARDIAL INFARCTION
BETA BLOCKERS | USES
management of ____
angina pectoris
stable heart failure - by blocking renin
BETA BLOCKERS | USES
drugs used for management of STABLE heart failure
Bisoprolol
Carvedilol
Metoprolol succinate
Nebivolol
BETA BLOCKERS | USES
management of ____ EXCEPT Sotalol
arrhythmia
BETA BLOCKERS | USES
for eye disorders
Timolol
Betaxolol
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
BETA BLOCKERS | USES
ENDOCRINE D/O:
can be sedating
Propranolol
BETA BLOCKERS | USES
ENDOCRINE D/O:
less sedating
Carvedilol
problem with hyperthyroidism
high levels of T3
BETA BLOCKERS | USES
- prophylaxis of migraine
- tx of stage fright
- symptomatic treatment of alcohol withdrawal
- used in infantile hemangiomas (birthmark)
PROPRANOLOL
BETA BLOCKERS
TOXIC EFFECTS
- bradycardia
- mask hypoglycemic symptom (tachycardia)
- bronchoconstriction
- hyperlipidemia (by blocking b3)
MAIN NT of Parasympathetic drugs
ACETYLCHOLINE
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
BIOSYNTHESIS:
active uptake of ____
choline
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
BIOSYNTHESIS:
choline entry in ____
presynapse
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
BIOSYNTHESIS:
rate limiting step
active uptake of choline
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
BIOSYNTHESIS:
transporter
choline transporter
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
BIOSYNTHESIS:
choline transporter inhibitor
Hemicholinium
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
FORMATION:
combine with ____ from mitochondrion
acetyl CoA
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
FORMATION:
catalyzing enzyme
choline acetyl transferase
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
STORAGE:
entry to vesicles through ____
VAT: vesicle associated transporter
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
STORAGE:
VAT inhibitor
Vesamicol
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
RELEASE:
exocytosis enhancer
a-latrotoxin
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
RELEASER:
exocytosis inhibitor
botulinumtoxin
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
TERMINATION:
enzyme for metabolism
acetylcholinesterase
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
TERMINATION:
hydrolyze Ach to chloine and acetate
AChE
PARASYMPATHETIC DRUGS | ACETYLCHOLINE
TERMINATION:
AChE is inhibited by
anticholinesterase
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | MUSCARINIC
- in the parietal cell
- activate proton pump –> HCl production
- ACIDITY
M1
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | MUSCARINIC
- in the atria of the heart
- bradycaria
M2
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: bronchoconstriction
- GIT: bowel movement
- URINARY BLADDER: urination
M3
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC
- ganglion –> synaptic neurotransmission
- adrenal medulla –> EPI release
NICOTINIC Neural (N)
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC
NICOTINIC NEURAL:
synaptic neurotransmission
ganglion
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC
NICOTINIC NEURAL:
EPI release
adrenal medulla
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC
- neuromuscular end plates –> skeletal muscle contraction
NICOTINIC MUSCULAR (M)
PARASYMPATHETIC DRUGS | CHOLINOCEPTORS | NICOTINIC
NICOTINIC MUSCULAR:
skeletal muscle contraction
neuromuscular end plates
PARASYMPATHETIC DRUGS
AGONIST
Cholinomimetics
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS
- cholinoceptor activation: drug binding
DIRECT ACTING
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
CHOLINE ESTERS:
* ACTIVATE muscarinic and nicotinic receptor
* Acetylcholine
* Carbachol
* Methacholine
NONSELECTIVE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
CHOLINE ESTERS:
NONSELECTIVE
Acetylcholine
Carbachol
Metacholine
ACM
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
CHOLINE ESTERS | NONSELECTIVE:
* bronchoconstrictor
* diagnostic agent in patient with suspected bronchial asthma: pulmonary challenge test
Methacholine
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
CHOLINE ESTERS:
* Bethanechol (Urecholine)
MUSCARINIC SELECTIVE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
CHOLINE ESTERS | MUSCARINIC SELECTIVE:
* management in the tx of urine retention
Bethanechol (Urecholine)
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
ALKALOIDS:
nonselective
Arecoline
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
ALKALOIDS:
muscarinic selective
Muscarine
Pilocarpine
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
ALKALOIDS | MUSCARINIC SELECTIVE:
* for mgt of glaucoma
* for mgt of GI atony (no contraction)
PILOCARPINE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
ALKALOIDS:
* for mgt of smoking cessation
* Nicotine
* Lobeline
* Varenicline
NICOTINIC SELECTIVE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | DIRECT ACTING
ALAKLOIDS | NICOTINIC SELECTIVE:
* NOT FDA approved
Lobeline
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS
- inhibit Ach metabolism = enhance ACh for action
- aka anticholinesterase
INDIRECT acting
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
- SAFE
- Aminoalcohol
- Carbamates
REVERSIBLE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
REVERSIBLE:
aminoalcohol
Edrophonium (Tensilon)
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
REVERSIBLE:
carbamates
Physostigmine/Eserine
Pyridostigmine
Neostigmine
Ambenonium
Demecarium
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
REVERSIBLE | CARBAMATES:
BRAND NAME of Physostigmine
Eserine
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
ORGANOPHOSPHATES
IRREVERSIBLE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
IRREVERSIBLE:
Agricultural poision (Insecticides)
Malathion, Parathion
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
IRREVERSIBLE:
nerve gases
Soman
Tabbun
Sarin
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
IRREVERSIBLE:
ONLY clinically useful
Echothiophate
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT ACTING
Tacrine
Donepezil
Galantamine
Rivastigmine
CNS acting
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
management for ____
alzheimer’s disease
myasthenia gravis
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
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
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
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
ALZHEIMER’S DISEASE:
general effect
low Ach
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
ALZHEIMER’S DISEASE:
treatment
CNS acting cholinergics –> increase ACh effects
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
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
MYASTHENIA GRAVIS:
symptom
ptosis of the left eye
(drooping eyelids)
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
MYASTHENIA GRAVIS:
diagnosis
Edrophonium (Tensilon test(
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
MYASTHENIA GRAVIS:
treatment
carbamates
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
management for glaucoma; lower IOP
Echothiophate
Demecarium
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
GI atony
Physostigmine
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
ANTIDOTES:
* for Atropine poisoning
* can enter the brain targeting both central & peripheral
PHYSOSTIGMINE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
ANTIDOTES:
* for other anticholinergic poisoning
NEOSTIGMINE
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT | CLINICAL USE
ANTIDOTES:
* for NMB toxicity
Edrophonium + Neostigmine
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT
TOXIC EFFECTS
DUMBBELSS
diarrhea, urination, miosis, bradycardia, bronchoconstriction, emesis, lacrimation salivation, sweating
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT
TREATMENT FOR TOXIC EFFECTS:
Early (short)
cholinesterase activators
Pralidoxime
Diacetylmonoxime
PARASYMPATHETIC DRUGS | CHOLINOMIMETICS | INDIRECT
TREATMENT FOR TOXIC EFFECTS:
Late (long)
anticholinergic
Atropine
PARASYMPATHETIC DRUGS
ANTAGONISTS
CHOLINOLYTICS
PARASYMPATHETIC DRUGS | CHOLINOLYTICS
ANTIMUSCARINIC/ANTICHOLINERGIC:
prototype
ATROPINE
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
pharmacologic effects of ATROPINE
sympathetic effect
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS:
M1 blockade
inhibit HCl production
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS:
M2 blockade
tachycardia
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS | M3 blockade:
EXOCRINE GLANDS
DRYNESS - xerostomia, anhidrosis, hyperthermia, erythema
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS | M3 blockade:
SMOOTH MUSCLES
relaxation
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS | M3 blockade:
EYES: ciliary
cycloplegia
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS | M3 blockade:
EYES: muscles
mydriasis
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS | M3 blockade:
bronchi
bronchodilation
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS | M3 blockade:
GIT
ileus
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
PERIPHERAL EFFECTS M3 blockade:
urinary bladder
retention
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
- tx for symptomatic BRADYCARDIA
- tx of CHOLINOMIMETIC poisoning
- given with diphenoxylate as antidiarrheal
- adjunct treatment for parkinsonism
- antispasmodic
ATROPINE
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
ATROPINE is given with ____ as antidiarrheal to lessen addiciton
diphenoxylate
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
CNS ACTING:
* mgt of extrapyrimidal syndrome (SE of antipsychotics)
* mgt of parkinsonism
Benztropine
Biperiden
Trihexyphenidyl
BBT
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
CNS ACTING:
* used in the tx of motion sickness
scopalamine
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
EYE ACTING:
* for eye exam
Mydriatics
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
EYE ACTING:
* tx of pain during eye injury
* Homatropine
* Anistropine
* Cyclopentolate
Cyloplegics
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
bronchi acting cholinergics causes
relaxation (dilation)
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
BRONCHI ACTING:
SHORT acting muscarinic antagonist (SAMA)
Ipratropium
Oxytropium
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
BRONCHI ACTING:
LONG acting muscarinic antagonist (LAMA)
Tiotropium
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
GASTRIC GLAND ACTING:
* mgt of hyperacidity
Pirenzepine
Telenzepine
PARASYMPATHETIC DRUGS | CHOLINOLYTICS | ANTIMUSCARINIC/ANTICHOLINERG
GIT & URINARY BLADDER ACTING:
* for mgt of urine incontinence, hypermotility
Methscopalamine
Glycopyrolate
HNBB
Dicycloverine
Oxybutinin
Scopalamine
PARASYMPATHETIC DRUGS | ANTINICOTINIC
- Ganglionic blockers
- obsolete antihypertensive
- Hexamethonium, Trimethaphan, Mecamylamine
NN blockers
PARASYMPATHETIC DRUGS | ANTINICOTINIC
NN blockers
Hexamethonium
Trimethaphan
Mecamylamine
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
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
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS
DEPOLARIZING / IRREVERSIBLE / NONCOMPETITIVE:
INITIAL effect
depolarization & overstimulation of NM receptor
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
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
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
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING
SUCCINYLCHOLINE:
DOA
3-5 mins
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING
SUCCINYLCHOLINE:
given by
IV infusion
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING
SUCCINYLCHOLINE:
order of paralysis
- Fasciculations in chest & abdomen
- Neck, arms, legs
- Facial, pharynx, larynx
- Respiratory muscles
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING
TOO LONG duration of action
Decamethonium
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKERS | DEPOLARIZING
Action is shorter than decamethonium since it is rapidly metabolized by cholinesterase
Suxamethonium
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
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | NONDEPOLARIZING
ISOQUINOLINE
curium
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | NONDEPOLARIZING
STEROIDAL
curonium
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS
GENERAL
skin wheals
transient hypotension
tachy brady
respiratory/diaphragmatic paralysis
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS
SUCCINYLCHOLINE
myalgia, myositis
rhabdomyolysis
malignant hypothermia
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS
TUBOCURARINE
increase degranulation leading to anaphylactoid reaction
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER |TOXIC EFFECTS
TUBOCURARINE TOXICITY:
treatment
Epinephrine
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
PARASYMPATHETIC DRUGS | ANTINICOTINIC | NM BLOCKER | REVERSAL
- antagonizes NEUROMUSCULAR BLOCKADE purely by inhibiting acetylcholinesterase activity
EDROPHONIUM
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