BIO200H5 Lecture Notes - Lecture 10: Biotransformation, Hydrophile, Bioavailability

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9 Nov 2018

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Sometimes drugs that you take are not the active form, so sometimes metabolism can lead to the active form of the drug: the metabolites that we have will now be eliminated because they are easier to eliminate. Some drugs can be administered as active compounds and be effective right away. Some might undergo a very fast elimination: talking about a very hydrophilic drug (any type of administration) It will be absorbed right away and taken care of right away by the kidney, so we need a higher dose and if we give a higher dose, then we might have a toxic off-target effect. Some drugs might have a severe first pass effect. If drug is given orally and be absorbed in the gut lumen or metabolize in the liver: there will be very low bioavailability. If drug is taken orally, there will be a first pass effect in the liver or the kidney.

Related Questions

Need help with biology questions:

1. To increase the excretion of an acidic drug, what would you do to the urine?

	A.	Make it more basic
	B.	None of the above
	C.	Make it neutral
	D.	Make it more acidic

2. G-Protein coupled receptors directly act on which of the following secondary messenger molecules:

	A.	cAMP
	B.	ATP
	C.	ADP
	D.	GTP
	E.	None of the above or more than one of the above

3. Drug A and Drug B both produce the same level of biological/physiological response. Drug A produces this effect with 100 mg/kg dose. Drug B produces this effect with 50 mg/kg dose. Which of the following is true?:

	A.	Drug B is more efficacious than Drug A. Both drugs are equally potent.
	B.	Drug A is more efficacious than Drug B. Both drugs are equally potent.
	C.	Drug A and B are equally efficacious. Drug A is more potent than Drug B.
	D.	Drug A and B are equally efficacious. Drug B is more potent than Drug A.

4. The stomach has a ______ pH, whereas the small intestines have a _______ pH. The colon has an approximately ___________ pH.

	A.	High; low; neutral
	B.	Low; high; neutral
	C.	Low; neutral; neutral
	D.	None of the above

5. Which receptor is most likely to reduce norepinephrine levels when activated?

	A.	alpha 2 adrenergic
	B.	alpha 1 adrenergic
	C.	dopamine D1 receptors

6. Which of the following statements are FALSE?

	A.	If the Vd of a drug is between 60 and 80 L the drug has likely distributed to the total body water of a 200 kg man.
	B.	In the enterohepatic system the activity of bacteria to remove conjugates from a drug in the gut will decrease the clearance of the drug.
	C.	Lipid drugs are more likely to be reabsorbed by the kidney from the urine.
	D.	A weak basic drug (pKa = 6) will be mostly ionized in urine of a pH= 3 and only the non- ionized drug will be eliminated.
	E.	The major conjugate in Phase 2 metabolism is glucuronide.

7. Isoproterenol (Î²-agonist) is a vasodilator that increases HR. What happens to systolic and diastolic pressures upon IV administration of isoproterenol?

	A.	â systolic; â diastolic
	B.	â systolic; â diastolic
	C.	â systolic; â diastolic
	D.	â systolic; â diastolic
	E.	None of the above

8. If you want to increase the blood concentration of a drug A, you can perform which of the following procedures:

	A.	Inhibit Drug A metabolism with Drug B
	B.	Enhance Drug A reabsorption from renal proximal tubule by changing ionization of Drug A with Drug B
	C.	Allow competition of Drug B with Drug A for active renal secretion processes
	D.	Increase the binding of Drug A to serum albumin
	E.	All of the above

9. Which of the following describes Phase I metabolism?

	A.	Inactive products are always produced in this phase.
	B.	Large molecules such as glucuronic acid are conjugated to drugs in this phase.
	C.	This phase may produce active metabolites from prodrugs.
	D.	This phase only occurs in the liver.

10. Which of the following is NOT an enzyme involved in the biosynthesis of biogenic amines?

	A.	Phenylethanolamine N-methyl Transferase
	B.	Dopamine Î²-hydroxylase
	C.	Tyrosine dehydroxylase
	D.	DOPA decarboxylase
	E.	All of the above

11. Why would an antibiotic at the same concentration be more active against bacteria in water than in serum or plasma? (Activity is measured in a test tube)

	A.	activity of the antibiotic is increased in water.
	B.	due to drug-protein interaction in serum
	C.	the antibiotic is more stable in water
	D.	all of the above
	E.	none of the above

12. Ion channels are targets for drugs. Which drug class targets Na+ channels?

	A.	Benzodiazepines
	B.	Beta blockers
	C.	Local anesthetics
	D.	Antihypertensive drugs (cardiac and smooth muscle)
	E.	Glibenclimide (diabetic drug)

13. _________________ not metabolized by catechol-O-methyltransferase (COMT).

	A.	Dopamine
	B.	Epinephrine
	C.	Phenylephrine
	D.	Norepinephrine
	E.	All of the above are metabolized by COMT.

Case Study Section 4 â Nitrogen Metabolism Based on âA Sickeningly Sweet Baby Boy: A Case Study on Autosomal Recessive Inheritanceâ by Jacqueline Washington and Anne Zayaitz (National Center for Case Study Teaching in Science) The Patient: Mathew Miller is a 7-day-old infant that is rushed to the emergency room by his parents Emma and Jacob Miller, Mennonites from Lancaster County, PA. Emmaâs pregnancy and delivery with Mathew was normal but he started having trouble nursing and now has completely stopped feeding. By the time they reach the emergency room Mathewâs limbs were rigid and he had had a seizure. The initial examination showed no infection and his x-rays were normal. The family history collected by the Doctor revealed that Emma and Jacob had had a previous son, Samuel that died at 9 days-of-age. There also is a history of unexplained childhood mortality on both sides of the family; Emmaâs mother had two sisters who died in the first year of their lives and Jacobâs father had a sister who died at 7 months of age. Emma also points out to the Doctor that Mathewâs diaper has a funny smell to it. Blood and urine samples were taken for testing and skin biopsies from Mathew, Emma, and Jacob were taken and tested for enzyme activity. The tests results showed that:

â¢ Mathewâs urine had elevated levels of the branched chain amino acids and their Î±-keto acid derivatives (which caused the sweet smell in his diapers)

â¢ Both Emma and Jacobâs skin biopsies had nearly normal levels of branched chain amino acid metabolism/enzyme activity

â¢ Mathewâs enzyme activity was less than 2% of normal

Question 1: What is the most likely diagnosis for Mathew?

A. Argininemia

B. Diabetes mellitus '

C. Maple syrup urine disease

D. Phenylketonuria

Question2: What enzyme did the skin biopsy test measure?

A. Carbamoyl phosphate synthetase I

B. Alanine aminotransferase

C. Phenylalanine hydroxylase

D. Branched-chain Î±-keto acid dehydrogenase complex

Question 3: This enzyme functions VERY similarly to two other enzymes that we have discussed, what are they?

A. Phosphofructokinase-1 and fructose 1,6-bisphosphatase (FBPAse-1)

B. Pyruvate dehydrogenase complex and Î±-ketoglutarate dehydrogenase complex

C. Urease and arginase

D. Isocitrate dehydrogenase and malate dehydrogenase

Question 4: How did Mathew (and presumably Samuel) inherit the disease if both Emma and Jacob have normal enzyme activity levels?

A. Emma and Jacob must both be carriers for the disease but their one normal gene is enough to maintain enzyme activity levels.

B. The disease can happen spontaneously, there is no genetic link.

C. Jacob is not really the father of the boys.

D. The disease can skip generations.

Question 5: What would be the best diet for Mathew to follow to control his disease?

A. Atkinâs diet (low carbohydrates, high fat, and high protein)

B. Low protein

C. Low fat

D. No special diet will control the disease

Over the next 4 years Mathewâs metabolic disease is controlled by his special diet but he still suffers approximately 3 metabolic crises a year. These occur when amino acids accumulate in his blood leading to the swelling of his brain. Even something as simple as a cold or the flu can affect his amino acid levels and send his metabolism into crisis. Jacob and Emma decide that âWe cannot continue to live in constant fear that a minor infection or a simple cold or ear infection could kill our son. Even though we are doing everything we are supposed to, he is still getting sick and we are afraid we may lose Mathew.â They learn that some children with Mathewâs disease have undergone liver transplants and are effectively cured.

Question 6: How/why would a liver transplant effectively cure Mathewâs condition?

A. A new liver would be able to spread itâs genes throughout the body and correct the genetic disorder.

B. A new liver would more effectively respond to metabolic hormonal control.

C. A new liver would express the functional enzyme needed to metabolize the amino acids causing Mathewâs condition.

D. A new liver would produce more hemoglobin to transport oxygen more effectively.

The family is directed to Dr. Morton of Childrenâs Hospital of Pittsburgh, where transplant experts agree to list Mathew for a liver transplant. Jacob and Emma learn that children who receive a liver transplant have to take strong immunosuppressive drugs for the rest of their lives. It was also clear that there was a 40% possibility that Mathew could reject the liver and need a second transplant (which also might be rejected) or he could die from surgical complications.

Question 7: Assuming the liver transplant was successful and Mathew did not reject the new liver, what type of diet would Mathew be able to/need to eat?

A. He would still need to eat his special diet but he would be at less risk of a metabolic crisis

B. He could eat a normal diet

C. He would need to change to a high protein diet like Atkinâs

D. He would be on an all liquid diet

Question 8: Emma and Jacob decide they want to try to have another child. What would be the chance that this child would also have the disorder that Mathew and Samuel have/had?

A. 0 %

B. 25%

C. 50%

D. 75%

E. 100%

Question 9: If Mathew grew up, got married, and decided to have children, what would be the chance that his children would have the disorder? A. 0%, the liver transplant would have cured him

B. 25%

C. 50%

D. 100%

E. It would depend on his wife, if she was normal than there would be a 0% chance of his children having the disorder but 100% would be carriers, if she was a carrier than there would be a 50% chance of his children having the disorder and a 50% chance that they would be a carrier.

Question 10: The disorder is found in 1 in 200,000 infants throughout the US but 1 in 200 in the Amish and Mennonites of Lancaster County, PA. Why is there such a difference in the prevalence of the disease?

A. There are environmental factors associated with being Amish or Mennonites that increase the prevalence.

B. There is a large amount of genetic similarity within these populations because they tend to marry within the population so recessive disorders such as this are more likely.

C. The gene mutation is preferentially carried in Caucasians so when you average the prevalence across all races in the US the prevalence drops.

D. It is unknown why the prevalence is so much greater in Amish and Mennonites.

BIO200H5 Lecture Notes - Lecture 10: Biotransformation, Hydrophile, Bioavailability

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