Pharma Midterm 2 Flashcards
define a central muscle relaxant
relative specific depressant action on CNS
(causing decreased motor activity or paralysis of voluntary muscles without loss of consciousness)
Which CNS inhibitory drug demonstrate the strongest muscle relaxant effect
Phenotiazine
Which CNS inhibitory drug demonstrate the weakest muscle relaxant effect
Anaesthetics
What are the medical uses of muscle relaxant?
- central myorelaxants can potentiate the effect of anesthetics drugs and combinations
- used in control of certain spasmodic and painful disorders of skeletal (spinal) muscle
Give the main central muscle relaxant drugs?
- guaiphenesin
- baclofen
- Methocarbamol
- Carisoprodol
What is the indication for Guaiphenesin ?
- horse, cattle, sheep (with anaesthesia)
- équine tetanus, strychnine poisoning in dogs
What is baclophen mechanism of action ?
- GABAb agonist
indication of Baclophen?
- spasm of skeletal muscle
- spinal cord injury and pain caused by injuries
- use in dogs to treat urinary retention (reduces urethral resistance)
How is Carisoprodol used?
useful against various types of pain because of its potentiating effect on opioid analgesics
Indication for the use of Methocarbamol?
muscle inflammation, traumatic muscle spasm
Which ligand bounds to the nicotinic receptor
Acetycholine
What are the uses of neuromuscular blocking agents?
- adjuvant in surgical anaesthesia
- assist in intubation
- corneal or retinal surgeries to obtain relaxation of extra ocular muscles
- therapy of spastic disorder
with an IV or systemic administration
Give the main peripheral muscle relaxants?
- Suxamethonium
- Atracurium
- Pancuronium
- Rocuronium
- Vecuronium
- Tubocurarine
what are the undesirable side effects of depolarizing agents (peripheral muscle relaxants)?
- Bradycardia
- increased intra-ocular and intragastric pressure
- Anaphylaxis or malignant hyperthermia
What are the 2 groups of competitive neuromuscular blocking agents?
- Benzylisoquinoline (metabolised in blood plasma, HA release)
- Aminosteroid (metabolised in Liver, no HA release)
d- tubocurarine
long acting
HA release
excretion via urine
Atracurium
intermediate acting
safe in liver, kidney patients
not used in vet med
Sympahtetic nervous system
fight or flight
Parasympathetic nervous system
rest and digest
Transmitter for sympathetic nervous system?
norepinephrine
Where is the M2 muscarinic Ach receptors found, and what is its effect
heart
inhibition
Where are the M1, M3 Ach receptor found and what do they do?
- stomach, glands, bronchial smooth muscle, eye ciliary muscle (excitation)
- vascular endothelium (inhibition)
Give an antagonist to Acetylcholine
Atropine
Give a drug used against spasms
Atropine
effect of parasympathomimetics on the heart
negative chronotropic
effect of parasympathomimetics on the GI-tract
smooth muscle contraction
vomiting, diarrhea
effect of parasympathomimetics on the Resp tract
bronchoconstriction & increase bronchial secretion
effect of parasympathomimetics on the urinary tract
bladder contraction
What Is the difference between direction and indirect parasympathomimetics
direct : binds to Ach receptors
indirect: inhibition of Ach-esterase -> Ach degradation is reduced
Which parasympathomimetics is not used therapeutically
Acetylcholine
Which parasympathomimetics is only used locally, applied in uterus in case of metritis , and in glaucoma therapy as eye drops?
Carbachol
Which parasympathomimetics is a M-Ach R selective and used for urinary bladder atony?
Bethanechol
Which parasympathomimetics are M-Ach R selective?
Bethanechol
Methacholine
Mainly in human practice
Which parasympathomimetics are non-selective M-Ach R?
Acetylcholine
Carbachol
Give a direct parasympathomimetic, what
Pilocarpine
Used in ophthalmology :
- glaucoma therapy
- Keratoconjunctivitis sicca (KCS)
Give the indirect parasympathomimetics
Physostigmine
Pyridostigmine
Neostigmine
Which indirect parasympathomimetics has a very small therapeutic index systemically?
Physostigmine
Which indirect parasympathomimetics is used as a myasthenia gravis treatment given IV or IM
Neostigmine
Which indirect parasympathomimetics is used as a myasthenia gravis treatment given orally
Pyridostigmine
Which indirect parasympathomimetics is an irreversible inhibitor of AchE
Organophosphates
Which indirect parasympathomimetics is a competitive inhibition in neuromuscular junction and has a short effect
Edrophonium
How are Parasympatholytics used in the cardiovascular system
to lift cholinergic blockade of the heart
How are Parasympatholytics used for Resp tract
for bronchodilator and decrease mucus secretion
Why are Parasympatholytics used as premedication before surgery?
- antagonist bradycardia
- decrease saliva production
- decreasing bronchial secretion
- earlier inhalation anaesthetics
How can Parasympatholytics be used for therapy?
- eye treatment (short and long acting)
- bronchodilation (asthma)
- antidote in case of toxicoses (organophosphate toxicosis)
- antidiarrheal (ruminant)
- antispasmodics (used in colic horses)
Which specie is relatively resistant to atropine
Rabbit
Give the active substances of Parasympatholytics
- atropine (premedication)
- glycopyrrolate (premedication)
- homatropine (diagnostic eye exam)
- tropicamide (diagnostic eye exam)
- ipratropium (asthma)
- benzethimid (antidiarrheal)
- Butyl-scopolamine (antispasmodic)
What is the action of a1 receptor once activated
Smooth muscle contraction
Vasoconstriction
Mydriasis
What is the a2 receptor action once activated
Inhibition of NA Release
GI relaxation
Inhibition of insulin release
B1 receptor action
Cardiac, positive inotropic and chronotropic
B2 receptor action
Vasodilatation
Bronchodilatation
Uterus relaxation
B3 receptor action
Lipolysis in fat tissue
Cardiovascular effects of Sympathomimetics
+ chronotropic
+ inotropic
Vasodilation (b2 agonist)
Vasconstriction (a1 agonist)
Gastrointestinal effect of Sympathomimetics
Smooth muscle relaxation
GI Atony
Resp effects of Sympathomimetics
Bronchodilation
Decrease bronchial secretion
List the nonselective Sympathomimetics, and the receptors they act on
- adrenaline (b1,2 < a)
- noradrenaline (b1 and a1)
- dopamine ( D1 < b1< a1)
Give a Selective sympathomimetics for b1
Dobutamine, cardiogenic shock
Give a Selective sympathomimetics for b receptors
Isoproterenol
Give the b2 agonists
Clenbuterol
Salbutamole
Terbutaline
Salmeterole
Isoxsuprine
What happens if a b2 agonist is used in higher dosage
Acts on b1 receptors, cardiac effect
Indication to use b2 agonist
Horse RAO
feline asthma
Bronchitis, bronchopneumonia
Tracheal hypoplasia
Tracheal collapse
Give a Selective sympathomimetics of a1 R
Phenylephrine, vasoconstriction
Xylometazoline
Oxymetazoline
Naphazoline
Tetryzoline
Give a Selective sympathomimetics of a1 used for urinary bladder sphincter constriction
Phenylpropanolamine
What are the a2 agonist
Sedate hypnotics
- xylasine
- detomidine
- medetomidine
- romifidine
Give non selective a-antagonists
- phenoxybenzamine (urethra sphincter relaxation)
- phentolamine
- tolazoline
Give a1 antagonist
Prazosine
Doxasozine
a2 antagonist
Atipamezole
Yohimbine
B receptor antagonist
Propranolol
Timolol
B1 R antagonists
Metoprolol
Atenolol
Where is cortisole made in the body
Adrenal cortex
What is cortisol’s effect on the body
has a negative effect on Hypothalamus and hypophysis
What is the meaning of a glucocorticoid
glucose activated cortex steroid
Main physiological and pathological effect of glucocorticoid
stress hormone
diabetogenic
gluconeogenesis increase
muscle atrophy
decreased growth
polyuria/polydipsia
skin thinning
Pharmacological effects of glucocorticoids
anti inflammatory
antiallergic
immunosuppressive
antishock
neuroprotective
Where is the glucocorticoid’s receptor
intracellular
what is the mechanism of action of glucocorticoids
inhibits (cytokines) or induces certain genes
For what treatment would glucocorticoids be used in cats and horses?
asthma
Which mechanisms do glucocorticoid inhibits?
lipoxygenase (asthma)
Cyclooxygenase
Epoxigenase
How are glucocorticoids antiinflammatory and immunosuppressive drugs?
inhibits PLA2
inhibits expression of IL1-2-6
decrease TNF & IFN synthesis
apoptosis in lymphocytes
How do glucocorticoid have a neuroprotective effect?
NOT FOR BRAIN TRAUMA
counteract lipidperoxidation and enhance microcirculation
Which drug has for active substance acetate? how long does it act for?
Prednisolone, 5-6 days
Which drug has for active substance dipropionate? how long does it act for?
Betamethasone, 3 weeks
List the Glucocorticoids according to their potency
cortisol
Prednisolone
Methyprednisolone
Triamcinolone
Betamethasone
Dexamethasone
Beclomethason
Fluticason
Side effects of glucocorticoids
HT - hypophysis - adrenal cortex axis inhibition
gastric ulcers
hepatopathy (ALKP increase)
Pancreatitis
Glaucoma
Thinning of skin, delayed wound
Appearing of tumor
Polyphagia
Why would glucocorticoid be used in a high dosage
Only once, IV if
shock
spinal trauma
How could glucocorticoid Be used in an ADT
Using Prednisolone, methylprednisolone
every other day
How could glucocorticoid Be used in an ADT
Using Prednisolone, methylprednisolone
every other day
Which pathway do NSAIDs inhibit
Cylcooxigenase (COX)
PGF, PGE, PGI, TX
what’s the main physiological role of PGE, TXA
Stomach: intestine protection
decrease acid secretion
Blood clotting
Kidney : increased blood flow
What are the most important side effects of NSAIDs
renal toxicity
intestinal ulceration and ulceration
where can we find COX1 isoenzyme
stomach, kidney, platelets
(constitutive)
Where can we find COX2 isoenzyme
Macrophages
(Induced by inflammation)
What other name is there for acetaminophen?
Paracetamol
What are the main effect of paracetamol and metamizole
analgesic
antipyretic
NO ANTI INFLAMMATORY EFFECT
Ketoprofen and aspirin are also known as
Traditional NSAID drug
(mainly COX 1 inhibition)
Meloxicam, Carprofen, Deracoxib, Firocoxib are inhibiting which isoenzyme
COX 2
Give the drugs that act as COX 2 inhibition
Meloxicam, Carprofen, Deracoxib, Firocoxib
What are the pharmacological effects of NSAIDs
Anti Inflammatory
Analgesic
Antipyretic
Platelet aggregation inhibition (antiendotoxin, spasmolytic, antineoplastic)
Example of antiendotoxin drug?
Meloxicam
Meloxicam has for pharmacological effect?
Antiendotoxin