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stimulants
Respiratory stimulants
DEFINITION
It is defined as "the drug or chemical agent which is used to
stimulate the respiratory system or restore the normal respiration
when lungs are unable to eliminate sufficient amount of carbon
dioxide and unable to take sufficient amount of oxygen molecule
are collectively known as respiratory stimulant.
It include the class of those drug which is used to
•
stimulate the CNS i.e Central nervous system of the body,
hence it is known as CNS stimulator
Pharmacokinetics
Onset : 20 to 40 sec
Duration: 5-12 min(single IV ) Peak
Plasma Time: 1-2 min
Half-life: 3.4 hr (2.4-4.1 hr)
BRAND FORM.
20 mg/mL
Dopram
solution
20 mg/mL
doxapram
solution
Caffeine
Mechanism of Action
Methylxanthine; promotes cAMP (Cyclic adenosine monophosphate) accumulation
by inhibiting phosphodiesterase; increases medullary respiratory center sensitivity
to carbon dioxide; may prevent apnea by acting as an adenosine receptor
antagonist.
The CNS stimulant action of these drugs also contributes to improved respiratory
function, as also the improvement in circulatory and renal function in cardiac
asthma of dogs.
·
Pharmacokinetics
●Half-Life: 72-96hr
● Peak plasma time: 30-120 min
●Peak plasma concentration: 1.5-1.8 mcg/mL
●Protein Bound: 17-36%
●Vd: 0.6-0.9 L/kg
● Metabolism: hepatic CYP1A2
●Excretion: Urine
Dose:
Respiratory Failure
They make breathing easier for people with asthma or other lung conditions.
Bronchodilators include
(iii) theophylline.
(i) Beta-2 agonists
Example: epinephrine, salbutamol, levosalbutamol, isoprenaline
●Beta-2 agonists are available in short-acting and long-acting varieties, and are
usually taken through an inhaler.
●They relax the muscles in the lungs, which allows the airways to widen. Long-
acting beta-2 agonists can also reduce the amount of mucus in the lungs by
speeding up the motion of cilia. Cilia are tiny hairs that line the walls of airways
and help 'sweep' mucus out of the airways.
●In the lung, cAMP decreases calcium concentrations within cells and activates
protein kinase A. Both of these changes inactivate myosin light-chain kinaseand
activate myosin light-chain phosphatase.
●More severe effects, such as pulmonary edema, myocardial ischemia, and cardiac
arrhythmia, are exceptional.
(ii) Anticholinergic drugs
These nerve impulses are responsible for involuntary muscle movements in the:
●gastrointestinal tract
● lungs
● urinary tract
● other parts of your body
Side effects :
● dry mouth ● blurry vision
● Constipation ● drowsiness
● Sedation ● hallucinations
● memory problems ● trouble urinating
● Confusion ● delirium
● decreased sweating ● decreased saliva
(iii) Theophylline.
Theophylline is also used to treat both dogs and cats with collapsing trachea, intrathoracic
airway collapse and pulmonary edema.
●Derivatives of theophylline with superior pharmacokinetic properties are now
preferred.
●In man the corticosteroids are used for severe, disabling, bronchodilator-
resistant asthma.
●The introduction of NSAIDs with high antiinflammatory potency has made this
group beneficial as adjuncts along with antimicrobials.
● They lack the suppression of the immune response seen with the corticosteroids
.
●Their ability to suppress the production of the chemical mediators of the
inflammatory response underlies their ability to reduce structural damage and
functional impairment in the pneumonic lung.