Chapter 25: Drugs for Diabetes

Question 1

INSULIN

Answer 1

Insulin aspart NOVOLOG
Insulin detemir LEVEMIR
Insulin glargine LANTUS
Insulin glulisine APIDRA
Insulin lispro HUMALOG
NPH insulin suspension HUMULIN N,
NOVOLIN N
Regular insulin HUMULIN R, NOVOLIN R

Question 2

AMYLIN ANALOG

Answer 2

Pramlintide SYMLIN

Question 3

ORAL AGENTS

Answer 3

Acarbose PRECOSE
Glimepiride AMARYL
Glipizide GLUCOTROL
Glyburide DIAETA, GLYNASE PRESTAB
Metformin FORTAMET, GLUCOPHAGE
Miglitol GLYSET
Nateglinide STARLIX
Pioglitazone ACTOS
Repaglinide PRANDIN
Rosiglitazone AVANDIA
Saxagliptin ONGLYZA
Sitagliptin JANUVIA
Tolbutamide TOLBUTAMIDE

Question 4

INCRETIN MIMETIC

Answer 4

Exenatide BYETTA, BYDUREON
Liraglutide VICTOZA

Question 5

Rapid-acting and short-acting insulin preparations

Answer 5

regular insulin, insulin lispro
[LIS-proe], insulin aspart [AS-part], and insulin glulisine [gloo-LYSEeen].
Regular insulin is a short-acting, soluble, crystalline zinc insulin.
Insulin lispro, aspart, and glulisine are classified as rapid-acting insulins.
Modification of the amino acid sequence of regular insulin produces
analogs that are rapid-acting insulins. For example, insulin lispro
differs from regular insulin in that the lysine and proline at positions 28
and 29 in the B chain are reversed. This modification results in more
rapid absorption, a quicker onset, and a shorter duration of action after
subcutaneous injection. Peak levels of insulin lispro are seen at 30 to
90 minutes, as compared with 50 to 120 minutes for regular insulin.
Insulin aspart and insulin glulisine have pharmacokinetic and pharmacodynamic
properties similar to those of insulin lispro. Rapid- or
short-acting insulins are administered to mimic the prandial (mealtime)
release of insulin and to control postprandial glucose. They may also
be used in cases where swift correction of elevated glucose is needed.
Rapid- and short-acting insulins are usually used in conjunction
with a longer-acting basal insulin that provides control of fasting glucose.
Regular insulin should be injected subcutaneously 30 minutes
before a meal, whereas rapid-acting insulins are administered in the
15 minutes
proceeding a meal or within 15 to 20 minutes after starting
a meal. Rapid-acting insulins are commonly used in external insulin
pumps, and they are suitable for IV administration, although regular
insulin is most commonly used when the IV route is needed.

Question 6

Intermediate-acting insulin

Answer 6

Neutral protamine Hagedorn (NPH) insulin is an intermediate-acting
insulin formed by the addition of zinc and protamine to regular insulin.
[Note: Another name for this preparation is insulin isophane.] The
combination with protamine forms a complex that is less soluble,
resulting in delayed absorption and a longer duration of action. NPH
insulin is used for basal (fasting) control in type 1 or 2 diabetes and
is usually given along with rapid- or short-acting insulin for mealtime
control. NPH insulin should be given only subcutaneously (never IV),
and it should not be used when rapid glucose lowering is needed
(for example, diabetic ketoacidosis). Figure 25.8 shows common regimens
that use combinations of insulins.

Question 7

Long Acting Insulin Preparation

Answer 7

C. Long-acting insulin preparations
The isoelectric point of insulin glargine [GLAR-geen] is lower than
that of human insulin, leading to formation of a precipitate at the
injection site that releases insulin over an extended period. It has a
slower onset than NPH insulin and a flat, prolonged hypoglycemic effect with no peak (Figure 25.7). Insulin detemir [deh-TEE-meer] has
a fatty acid side chain that enhances association to albumin. Slow
dissociation from albumin results in long-acting properties similar to
those of insulin glargine. As with NPH insulin, insulin glargine and
insulin detemir are used for basal control and should only be administered
subcutaneously. Neither long-acting insulin should be mixed in
the same syringe with other insulins, because doing so may alter the
pharmacodynamic profile.

Question 8

Insulin combination

Answer 8

Various premixed combinations of human insulins, such as 70% NPH
insulin plus 30% regular insulin (Figure 25.8), or 50% of each of these
are also available. Use of premixed combinations decreases the number
of daily injections but makes it more difficult to adjust individual
components of the insulin regimen.

Question 9

std tx vs intensive treatment

Answer 9

Standard insulin therapy involves twice-daily injections. In contrast,
intensive treatment utilizes three or more injections daily with frequent
monitoring of blood glucose levels. The ADA recommends a
target mean blood glucose level of 154 mg/dL or less (HbA1c ≤ 7%),
and intensive treatment is more likely to achieve this goal. [Note:
Normal mean blood glucose is approximately 115 mg/dL or less
(HbA1c < 5.7%).] The frequency of hypoglycemic episodes, coma,
and seizures is higher with intensive insulin regimens (Figure 25.9A).
However, patients on intensive therapy show a significant reduction
in microvascular complications of diabetes such as retinopathy,
nephropathy, and neuropathy compared to patients receiving
standard care (Figure 25.9B). Intensive therapy should not be recommended
for patients with long-standing diabetes, significant microvascular
complications, advanced age, and those with hypoglycemic
unawareness. Intensive therapy has not been shown to significantly
reduce macrovascular complications of diabetes.

Question 10

synthetic amylin analog

Answer 10

Amylin is a hormone that is cosecreted with insulin from β cells following
food intake. It delays gastric emptying, decreases postprandial glucagon
secretion, and improves satiety. Pramlintide [PRAM-lin-tide] is a synthetic
amylin analog that is indicated as an adjunct to mealtime insulin therapy
in patients with type 1 and type 2 diabetes. Pramlintide is administered
by subcutaneous injection immediately prior to meals. When pramlintide
is initiated, the dose of mealtime insulin should be decreased by 50% to
avoid a risk of severe hypoglycemia. Other adverse effects include nausea,
anorexia, and vomiting. Pramlintide may not be mixed in the same
syringe with insulin, and it should be avoided in patients with diabetic
gastroparesis (delayed stomach emptying), cresol hypersensitivity, or
hypoglycemic unawareness.