Anticholinergic Drugs Flashcards
Anticholinergic drugs class
Competitive antagonists for Ach at muscarinic cholinergic receptors for in heart, salivary glands and smooth muscle of GI
Tertiary amine drug (2)
Atropine and Scopolamine
Quarternary amine drug
Glycopyrrolate
Which one types are unionized and cross BBB
Atropine
Scopolamine
Anticholinergic ONLY WORK at
MUSCARINIC receptors.
MOA of anticholinergic
combine reversibly with muscarinic receptors and
Prevent access of ACH to receptor site
Five subtypes of muscarinic
M1, M2, M3, M4, M5
Atropine affects
All Ms receptors
M1 found in
CNS and stomach
M2 found in
CNS and heart
M3 found in
Salivary glands
Airway smooth muscles
SALIVATION
M4 found in
CNS and heart
M5 found in
CNS
Effects on M2
Bradycardia
With those agents, doses needed to affect the heART.
Larger doses to affect the heart.
FIRST EFFECTS OF ANTICHOLINERGIC IS ON
SALIVARY GLANDS
*****Comparative effects : Greatest and least effect Sedation\_\_\_\_\_\_\_\_\_\_ Antisialagogue \_\_\_\_\_\_\_\_\_ Heart Smooth muscle
Compare
Greatest SEDATIVE PROPERTY
SCOPOLAMINE
NO sedative
GLYCOPYRROLATE
If you don’t want any HR increase or stimulation
GLYCOPYRROLATE
GREATEST effects on heart
ATROPINE
You don’t want Any IOP (avoid in glaucoma)
GLYCOPYRROLATE
Worst effect on IOP (increase)
SCOPOLAMINE
Motion- induced sickness BEST
SCOPOLAMINE
Motion sickness WORST
GLYCOPYRROLATE
100 times more potent than atropine as a sedating
SCOPOLAMINE
Not to be use in elderly, why?
SCOPOLAMINE; increase confusion, agitation
Fastest onset of action
1 minute
DOA 30-60 minutes
Does glycopyrrolate cross BBB? why not?
No; quaternary compound
Atropine metabolism and excretion
liver
urine
Anticholinergic use (2)
Prevent bradycardia
Sedative and antisialalogue effects
Less effect on pupil size_______
Glycopyrrolate
They can use as _______
Bronchodilators because they BLOCK parasympathetic NS
Dose of scopolamine for sedation
0.3-0.5mg IM
Central anticholinergic syndrome
ranging from restlessness to somnolence
Elderly patients more sensitive
ESPECIALLY with SCOPOLAMINE
What can potentiate anticholinergic syndrome
VA
What agent to reverse CNS effects of tertiary amine?
PHYSOSTIGMINE 15-60mcg/kg
Anticholinergic can
Decrease barrier pressure
Atropine and glycopyrrolate can
Decrease LES pressure
TREATMENT of REFLEX-MEDICATED BRADYCARDIA
Atropine 15-70 mcg/kg IV
most rapid onset
Atropine use with _______reversal agent
EDROPHONIUM
Glycopyrrolate use with _______reversal agent
NEOSTIGMINE
ATROVENT
Derivative of atropine
Quarternary compound
slow onset of action
Less effective than albuterol
Anticholinergic in the eye causes
MYDRIASIS and CYCLOPLEGIA
Patients with GLAUCOMA should not be given
SCOPOLAMINE
Anesthesia implications : SCOPOLAMINE
Effective in tx of N/V associated with morphine PCA and epidurals
Prophylactive TD scopolamine
applied evening before decreases nausea associated with laparoscopy in GA.
Symptoms of Anticholinergic OVERDOSE
Dry mouth Blurred vision Photophobia TACHYCARDIA Dry flushed ksin Rashes
Treatment of OVERdose is
Physostigmine 15-60 mcg/kg IV
Symptoms CNS overdose
CNS
Seizures, coma and medullary ventilatory center paralysis
