Carvedilol is a non-selective beta blocker with alpha blocker activity that can be used in management of heart failure and left ventricular dysfunction.
Hi everyone today in this video we are going to discuss about carbide all what is this drug carbonyl the suffix law indicates this drug is a non-selective beta blocker but this drug is also having additional activity so this drug is having nonsense to beta blocker activity along with alpha blocker activity so carbide all is both alpha and beta blocker normally the
Beta blockers are having a suffix whole all but within this name of this track we cannot identify the suffix all all o is not present instead we can take the suffix as dialog as usual the suffix law indicates this drug is a beta blocker and the term die can be remembered as this drug can act on both of the adrenergic receptors so along with beta blocker activity
This drug also acts as alpha blocker so the suffix dialog indicates this drug is a both alpha and beta blocker similarly within the name we can identify the prefix car this car indicates this drug is having carbohydrate system so carbadylol is a carbajal ring containing alpha and beta blocker what is the use of the strand this carbonyl can be used in the management
Of chronic heart failure where these drug blocks beta adrenergic receptors thereby reduce the cardiac work resulting in the improvement of symptoms in the patients similarly this drug can also be used in the patients with left ventricular dysfunction particularly this condition can be observed after acute myocardial infarction so the post myocardial infarction the
Patients may have left winter clot dysfunction with ejection fraction less than or equal to 40 percent in such patients carbon law can be given again to reduce the cardiac work as well as to increase the systemic circulation by vasodilation and finally this can also be used in the management of hypertension because this drug acts as a vasodilator by blocking alpha
Receptors now let’s see how this drug acts corporate law just we have discussed it can act on both beta receptors so particularly it can act on beta 1 receptors which are expressed on the cardiac system so that it can reduce the rate of contraction as well as force of contraction and when both rate as well as force of contraction are reduced cardiac work is also
Reduced that’s why this drug can be used in the treatment of heart failure as well as left ventricular dysfunction similarly this type can also act on the alpha 1 receptors which are expressed on the vascular smooth muscle by blocking these alpha receptors you can produce vasodilation that’s why this drug acts as antihypertensive being non-selective beta blocker
This drug can also act on beta2 receptors so that you can produce mixed type of sympathetic actions it can affect the glucose as well as thyroid hormone levels now that is the action of carbodylol on the cardiac on the heart beta 1 receptors are present which are g protein coupled receptors coupled with alpha beta gamma subunits when the norepinephrine binds to
These beta 1 receptors these receptors are activated such that they can activate 89 cyclist system ac now this adrenaline cyclist can convert the atp into one of the important secondary messenger cyclic amp this cyclic kmp plays an important role within the cardiac system to produce a contraction it can activate a group of phosphorylating enzymes protein kinase
A which are responsible for release of calcium from the sarcoplasmic reticulum as well as increased calcium permeability by all of these the cache elements within the heart are going to be increased now this calcium can act on the actin myosin complex when the calcium binds to troponin complex it can remove the troponin such that aggregate myosin filaments can
Slide on each other to produce contraction of the cardiac muscle in this way norepinephrine can produce a cardiac contraction resulting in the increased rate as well as force of contraction of the heart varuval is a non-cell to beta blocker with alpha blocker activity because of beta-blocking activity now this drug can bind to these beta-1 receptors expressed on
The heart by inhibition of these beta-1 receptors it can inhibit the contraction of the cardiac system so that the rate as well as force of contraction can be reduced in this way carbonyl can reduce the cardiac work thereby it can reduce the angina or any myocardial infarction and it also improves the cardiac efficiency by reducing the cardiac oxygen consumption
Second one it can also act on the vascular smooth muscle now vascular smooth muscle is expressed with alpha one adrenergic receptors these alpha one hydrogen receptors are again g protein coupled receptors coupled with alpha beta gamma subunits now norepinephrine can again bind to this alpha receptors when norepinephrine binds to these alpha receptors it can activate
Phospholipase system plc this phospholipase is a cleavage enzyme which can convert the phosphoryl ionostal biphosphate into ip3 uninstall triphosphate plus dhg diazel glycerol now this diesel glycerol can activate few of the phosphorylating enzymes protein kinase c which are going to increase the permeability of inward going calcium channels now the calcium can
More enter into the vascular smooth muscle and ip3 can also release the intracellular calcium so that intracellular cation levels are increased which produce contraction of the vascular smooth muscle in this way norepinephrine can produce vasoconstriction thereby can increase the blood pressure now carbodylol is a beta blocker with alpha blocker activity it can
Block the alpha 1 receptors so that you can inhibit the contraction resulting in vasodilation in this way carburetor can reduce the blood pressure that’s why it is used as antihypertensive waste range now that is the precautions of carbonyl oil this drug carbonyl can act through the beta 1 receptors so it can inhibit the sympathetic on the heart as sympathetic
Activity is reduced it can reduce the rate of contraction as well as force of contraction but when this drug is used at high dose it can produce more pronounced effect on the force of contraction so when the force of contraction is significantly reduced it can produce the worsening of heart failure and the fluids are retained because of reduced force of contraction
And reduced capillary permeability in such conditions we can give the diuretics such as furosemide in order to contract this decreased force of contraction because dietary can reduce the body volume so that the symptoms of heart failure can be improved that’s why this structure be carefully used in the high dose and should be started from the low dose and the
Dose should be gradually increased similarly this drug should not be stopped suddenly because it can produce worsening of heart failure as well as precipitation of angina because of increased sympathetic activity similarly this can also act on the beta2 receptors which are present on the respiratory system so by blocking these beta2 receptors it can reduce the
Bronchodilation mediated through the beta to receptors so this can result in the bronchospasm in the patients which is common with most of the non-selective beta blockers and particularly in the patients with chronic bronchitis bronchial inflammation or emphysema in such conditions this bronchospasm is more pronounced with use of carbonyl similarly carbon dioxide
Action through the beta 1 receptors it can block the synthetic activity on the heart thereby can reduce the rate of contraction resulting in the bradycardia as one of the important effects of the patients so the pulse rate is going to be reduced in the patients and when this pulse rate is going to be reduced by 55 then care should be taken and the dose of the drug
Should be reduced similarly this trek can block the alpha receptors so that it can block the sympathetic action on the vascular smooth muscle resulting in vasodilation and hypotension so hypotension is another important precaution that should be considered this carbonyl and it can produce sometimes postural hypotension so care should be taken when the study is
Prescribed particularly at high dose for longer periods catecholamines like epinephrine and norepinephrine can control the glucose levels they can act on the liver such that they can produce hepatic glucose production so sympathetic system can increase the glucose levels similarly they can also block the insulin release and when insulin is not released it can
Further increase the glucose levels in this way catecholamines can increase the glucose levels now carbodylol can block the actions of catecholamines thereby can produce a sudden hypoglycemia in the patients so care should be taken in the diabetic patients where the action of oral hypoglycemic agents are more pronounced with co-administration of carbohydrate but
At the same time this drug can also produce fluctuations of glucose levels and even it can produce hyperglycemia in few of the patients similarly carbonyl can increase the thyroid hormone levels resulting in the thyroid toxicosis and it can also increase the risk of pheochromocytoma this is a condition of adrenal tumor where it can produce severe hypertension
Due to release of catecholamines carbology can block alpha one receptors but still it can increase the risk of your chromosytoma similarly this can also increase the risk of peripheral vascular disease even it is having alpha blocker activity so fluctuation of any inhibition may result in increased risk of your chromosytoma and peripheral vascular disease in the
Patients now let’s see the side effects of carbide law this recommend you produce we have the side effects such as bradycardia hypotension fatigue syncope hyperglycemia and sometimes it can also produce hypoglycemia diarrhea dizziness headache asthenia lack of energy weight gain increasing the weight of the patients can be observed with this carbonyl all
Now that is the chemical nature of this diet so this is the structure of carbohydrate just like other beta blockers this carburetor is also having a same side chain which is attached to an aromatic ring system so let us give the membrane to the side chain this is one two and three so simply it is a propanol amine attached to the aryl group so carullon is again
Aryl oxy propanol amine now the mn group is present at the third portion so we can write this as three amino and oh group is present at the second portion so propane to all so three amino propane to all is attached to aryl group so it is a aryl oxy propanol amine but now this nitrogen of amine is having ethyl side chain so we can write this as two ethyl and
This ethyl group is having a phenoxy chain along with a methoxy group at the second portion so it can be represented as two methoxy phenoxy so that is a chain present on the amine group of the nitrogen similarly the aromatic ring system is nothing but the carboxyl which is attached at the first position so one dash nine h carbosol for i oxy it is attached to
The side chain by fourth position so that is the complete name of carbide law so cardiology just like the other beta blockers it is a aryl oxy propanolamine derivative how it is given this is available as tablet as well as capsule as a normal tablet as well as film coated tablet it is available and this is available in the different sense starting from 3.125 mg
Then doubling of this strength 6.25 mg 12.5 mg and 25 mg doubling of the strengths can be observed in the different types of tablets and the dose of the drug depends on the type of clinical indication in case of heart failure this rugged started at a low dose of 3.125 mg given twice daily but in case of hypertension or left ventricular dysfunction this can be
Used at initial dose of 6.25 mg again given twice daily and in both of the cases the dose can be slowly increased such that the maximum dose 25 mg can be achieved and the dose adjustment should be done after one to two weeks of the treatment so that’s about this drug carburyl which is a non-selective beta blocker with alpha blocker activity this drug blocks
Up beta receptors such that you can reduce the cardiac work resulting in the decreased rate and force of contraction that’s why bradycardia is one of the important precautions that should be considered with this carbonyl and it can also block alpha receptors resulting in the vasodilation leading to hypotension in the patients that’s why this drug can be used as
Antihypertensive agent along with other drugs such as diuretics so that’s about this carbodylol hope you have enjoyed this video if you like this video please subscribe to our channel share this video with your friends post your thumbs in the comment box thank you for watching this video
Transcribed from video
Carvedilol – Mechanism, precautions, side effects & uses By egpat
