PHARMACOLOGY 1
PHARMACOLOGY 1
PHARMACOLOGY 1
# Fig :-4.1
INTRODUCTION OF BLOOD SUGAR
Blood glucose, or blood sugar, is the main sugar found in your blood. It is your body's
primary source of energy. Your body breaks down most of that food into glucose and releases
it into your bloodstream. When your blood glucose goes up, it signals your pancreas to
release insulin. Insulin is a hormone that helps the glucose get into your cells to be used for
energy.
Diabetes is a disease in which your blood glucose levels are too high. When you have
diabetes, your body doesn't make enough insulin, can't use it as well as it should, or both. Too
much glucose stays in your blood and doesn't reach your cells .Normal range of sugar :-
• Two hours after the start of a meal: Less than 180 mg/dL
The most common way to check your blood glucose level at home is with a blood glucose
meter. A blood glucose meter measures the amount of glucose in a small sample of blood,
usually from your fingertip.
High blood glucose is called hyperglycemia . It is of two types -type 1 and type 2 diabeties.
Symptoms that your blood glucose levels may be too high include:
• Feeling thirsty
• Feeling tired or weak
• Headache
• Urinating (peeing) often
• Blurred vision
Hypoglycemia, also called low blood glucose, happens when your blood glucose level drops
below what is healthy for you . For many people with diabetes, this means a blood glucose
reading lower than 70 mg/dL. The symptoms can be different for everyone, but they may
include:
• Shaking
• Sweating
• Nervousness or anxiety
• Irritability or confusion
• Dizziness
• Hunger
Drugs used to treat hyperglycemia type 1 diabeties :-
1. Novorapid
2. Lantus
3. Novolin R
4. Humulin R
5. Aspart
Pharmacology of insulin Novorapid :-
NovoRapid is usually given immediately before a meal, although it may be given after
a meal if necessary. The usual dose is between 0.5 and 1.0 units per kilogram body
weight per day.
Insulin aspart binds to the insulin receptor (IR), a heterotetrameric protein consisting
of two extracellular alpha units and two transmembrane beta units. The binding of
insulin to the alpha subunit of IR stimulates the tyrosine kinase activity intrinsic to the
beta subunit of the receptor. The bound receptor autophosphorylates and
phosphorylates numerous intracellular substrates such as insulin receptor substrates
(IRS) proteins, Cbl, APS, Shc and Gab 1. Activation of these proteins leads to the
activation of downstream signaling molecules including PI3 kinase and Akt. Akt
regulates the activity of glucose transporter 4 (GLUT4) and protein kinase C (PKC),
both of which play critical roles in metabolism and catabolism. In humans, insulin is
stored in the form of hexamers; however, only insulin monomers are able to interact
with IR. Substitution of the proline residue at B28 with aspartic acid reduces the
tendency to form hexamers and results in a faster rate of absorption and onset of
action and shorter duration of action.
Pharmacodynamic of Novorapid :-
Insulin is a natural hormone produced by beta cells of the pancreas. In non-diabetic
individuals, a basal level of insulin is supplemented with insulin spikes following
meals. Postprandial insulin spikes are responsible for the metabolic changes that occur
as the body transitions from a postabsorptive to absorptive state. Insulin promotes
cellular uptake of glucose, particularly in muscle and adipose tissues, promotes
energy storage via glycogenesis, opposes catabolism of energy stores, increases DNA
replication and protein synthesis by stimulating amino acid uptake by liver, muscle
and adipose tissue, and modifies the activity of numerous enzymes involved in
glycogen synthesis and glycolysis. Insulin also promotes growth and is required for
the actions of growth hormone (e.g. protein synthesis, cell division, DNA synthesis).
Insulin aspart is a rapid-acting insulin analogue used to mimic postprandial insulin
spikes in diabetic individuals. The onset of action of insulin aspart is 10-15 minutes.
Its activity peaks 60-90 minutes following subcutaneous injection and its duration of
action is 4-5 hours.